1.
PubChem
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PubChem is a database of chemical molecules and their activities against biological assays. The system is maintained by the National Center for Biotechnology Information, a component of the National Library of Medicine, PubChem can be accessed for free through a web user interface. Millions of compound structures and descriptive datasets can be downloaded via FTP. PubChem contains substance descriptions and small molecules with fewer than 1000 atoms and 1000 bonds, more than 80 database vendors contribute to the growing PubChem database. PubChem consists of three dynamically growing primary databases, as of 28 January 2016, Compounds,82.6 million entries, contains pure and characterized chemical compounds. Substances,198 million entries, contains also mixtures, extracts, complexes, bioAssay, bioactivity results from 1.1 million high-throughput screening programs with several million values. PubChem contains its own online molecule editor with SMILES/SMARTS and InChI support that allows the import and export of all common chemical file formats to search for structures and fragments. In the text search form the database fields can be searched by adding the name in square brackets to the search term. A numeric range is represented by two separated by a colon. The search terms and field names are case-insensitive, parentheses and the logical operators AND, OR, and NOT can be used. AND is assumed if no operator is used, example,0,5000,50,10 -5,5 PubChem was released in 2004. The American Chemical Society has raised concerns about the publicly supported PubChem database and they have a strong interest in the issue since the Chemical Abstracts Service generates a large percentage of the societys revenue. To advocate their position against the PubChem database, ACS has actively lobbied the US Congress, soon after PubChems creation, the American Chemical Society lobbied U. S. Congress to restrict the operation of PubChem, which they asserted competes with their Chemical Abstracts Service
2.
Chemical formula
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These are limited to a single typographic line of symbols, which may include subscripts and superscripts. A chemical formula is not a name, and it contains no words. Although a chemical formula may imply certain simple chemical structures, it is not the same as a full chemical structural formula. Chemical formulas can fully specify the structure of only the simplest of molecules and chemical substances, the simplest types of chemical formulas are called empirical formulas, which use letters and numbers indicating the numerical proportions of atoms of each type. Molecular formulas indicate the numbers of each type of atom in a molecule. For example, the formula for glucose is CH2O, while its molecular formula is C6H12O6. This is possible if the relevant bonding is easy to show in one dimension, an example is the condensed molecular/chemical formula for ethanol, which is CH3-CH2-OH or CH3CH2OH. For reasons of structural complexity, there is no condensed chemical formula that specifies glucose, chemical formulas may be used in chemical equations to describe chemical reactions and other chemical transformations, such as the dissolving of ionic compounds into solution. A chemical formula identifies each constituent element by its chemical symbol, in empirical formulas, these proportions begin with a key element and then assign numbers of atoms of the other elements in the compound, as ratios to the key element. For molecular compounds, these numbers can all be expressed as whole numbers. For example, the formula of ethanol may be written C2H6O because the molecules of ethanol all contain two carbon atoms, six hydrogen atoms, and one oxygen atom. Some types of compounds, however, cannot be written with entirely whole-number empirical formulas. An example is boron carbide, whose formula of CBn is a variable non-whole number ratio with n ranging from over 4 to more than 6.5. When the chemical compound of the consists of simple molecules. These types of formulas are known as molecular formulas and condensed formulas. A molecular formula enumerates the number of atoms to reflect those in the molecule, so that the formula for glucose is C6H12O6 rather than the glucose empirical formula. However, except for very simple substances, molecular chemical formulas lack needed structural information, for simple molecules, a condensed formula is a type of chemical formula that may fully imply a correct structural formula. For example, ethanol may be represented by the chemical formula CH3CH2OH
3.
Jmol
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Jmol is computer software for molecular modelling chemical structures in 3-dimensions. Jmol returns a 3D representation of a molecule that may be used as a teaching tool and it is written in the programming language Java, so it can run on the operating systems Windows, macOS, Linux, and Unix, if Java is installed. It is free and open-source software released under a GNU Lesser General Public License version 2.0, a standalone application and a software development kit exist that can be integrated into other Java applications, such as Bioclipse and Taverna. A popular feature is an applet that can be integrated into web pages to display molecules in a variety of ways, for example, molecules can be displayed as ball-and-stick models, space-filling models, ribbon diagrams, etc. Jmol supports a range of chemical file formats, including Protein Data Bank, Crystallographic Information File, MDL Molfile. There is also a JavaScript-only version, JSmol, that can be used on computers with no Java, the Jmol applet, among other abilities, offers an alternative to the Chime plug-in, which is no longer under active development. While Jmol has many features that Chime lacks, it does not claim to reproduce all Chime functions, most notably, Chime requires plug-in installation and Internet Explorer 6.0 or Firefox 2.0 on Microsoft Windows, or Netscape Communicator 4.8 on Mac OS9. Jmol requires Java installation and operates on a variety of platforms. For example, Jmol is fully functional in Mozilla Firefox, Internet Explorer, Opera, Google Chrome, fast and Scriptable Molecular Graphics in Web Browsers without Java3D
4.
Simplified molecular-input line-entry system
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The simplified molecular-input line-entry system is a specification in form of a line notation for describing the structure of chemical species using short ASCII strings. SMILES strings can be imported by most molecule editors for conversion back into two-dimensional drawings or three-dimensional models of the molecules, the original SMILES specification was initiated in the 1980s. It has since modified and extended. In 2007, a standard called OpenSMILES was developed in the open-source chemistry community. Other linear notations include the Wiswesser Line Notation, ROSDAL and SLN, the original SMILES specification was initiated by David Weininger at the USEPA Mid-Continent Ecology Division Laboratory in Duluth in the 1980s. The Environmental Protection Agency funded the project to develop SMILES. It has since modified and extended by others, most notably by Daylight Chemical Information Systems. In 2007, a standard called OpenSMILES was developed by the Blue Obelisk open-source chemistry community. Other linear notations include the Wiswesser Line Notation, ROSDAL and SLN, in July 2006, the IUPAC introduced the InChI as a standard for formula representation. SMILES is generally considered to have the advantage of being slightly more human-readable than InChI, the term SMILES refers to a line notation for encoding molecular structures and specific instances should strictly be called SMILES strings. However, the term SMILES is also used to refer to both a single SMILES string and a number of SMILES strings, the exact meaning is usually apparent from the context. The terms canonical and isomeric can lead to confusion when applied to SMILES. The terms describe different attributes of SMILES strings and are not mutually exclusive, typically, a number of equally valid SMILES strings can be written for a molecule. For example, CCO, OCC and CC all specify the structure of ethanol, algorithms have been developed to generate the same SMILES string for a given molecule, of the many possible strings, these algorithms choose only one of them. This SMILES is unique for each structure, although dependent on the algorithm used to generate it. These algorithms first convert the SMILES to a representation of the molecular structure. A common application of canonical SMILES is indexing and ensuring uniqueness of molecules in a database, there is currently no systematic comparison across commercial software to test if such flaws exist in those packages. SMILES notation allows the specification of configuration at tetrahedral centers, and these are structural features that cannot be specified by connectivity alone and SMILES which encode this information are termed isomeric SMILES
5.
Drug
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A drug is any substance that, when inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue, causes a physiological change in the body. In pharmacology, a drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent. Traditionally drugs were obtained through extraction from plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a duration, or on a regular basis for chronic disorders. Another major classification system is the Biopharmaceutics Classification System and this classifies drugs according to their solubility and permeability or absorption properties. Psychoactive drugs are chemical substances that affect the function of the nervous system, altering perception. They include alcohol, a depressant, and the nicotine and caffeine. These three are the most widely consumed psychoactive drugs worldwide and are also considered recreational drugs since they are used for rather than medicinal purposes. Other recreational drugs include hallucinogens, opiates and amphetamines and some of these are used in spiritual or religious settings. Some drugs can cause addiction and all drugs can have side effects, excessive use of stimulants can promote stimulant psychosis. Many recreational drugs are illicit and international such as the Single Convention on Narcotic Drugs exist for the purpose of their prohibition. The transitive verb to drug arose later and invokes the psychoactive rather than properties of a substance. A medication or medicine is a drug taken to cure or ameliorate any symptoms of an illness or medical condition, the use may also be as preventive medicine that has future benefits but does not treat any existing or pre-existing diseases or symptoms. In the United Kingdom, behind-the-counter medicines are called pharmacy medicines which can only be sold in registered pharmacies and these medications are designated by the letter P on the label. The range of medicines available without a prescription varies from country to country, medications are typically produced by pharmaceutical companies and are often patented to give the developer exclusive rights to produce them. Those that are not patented are called generic drugs since they can be produced by other companies without restrictions or licenses from the patent holder, pharmaceutical drugs are usually categorised into drug classes. A group of drugs will share a chemical structure, or have the same mechanism of action. Another major classification system is the Biopharmaceutics Classification System and this groups drugs according to their solubility and permeability or absorption properties
6.
GABAA receptor
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The GABAA receptor is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid, the major inhibitory neurotransmitter in the nervous system. Upon activation, the GABAA receptor selectively conducts Cl− through its pore and this causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring. The reversal potential of the GABAA-mediated IPSP in normal solution is −70 mV, the active site of the GABAA receptor is the binding site for GABA and several drugs such as muscimol, gaboxadol, and bicuculline. The protein also contains a number of different allosteric binding sites which modulate the activity of the receptor indirectly, GABAA receptors occur in all organisms that have a nervous system. To a limited extent the receptors can be found in non-neuronal tissues, due to their wide distribution within the nervous system of mammals they play a role in virtually all brain functions. The ionotropic GABAA receptor protein complex is also the target of the benzodiazepine class of tranquilizer drugs. In addition peripheral benzodiazepine receptors exist which are not associated with GABAA receptors, in order for GABAA receptors to be sensitive to the action of benzodiazepines they need to contain an α and a γ subunit, between which the benzodiazepine binds. This potentiates the effect of the available GABA leading to sedative. Different benzodiazepines have different affinities for GABAA receptors made up of different collection of subunits, the much sought structure of GABAA receptor was finally resolved, with the disclosure of the crystal structure of human β3 homopentameric GABAA receptor. GABAA receptor is a transmembrane receptor that consists of five subunits arranged around a central pore. Each subunit comprises four transmembrane domains with both the N- and C-terminus located extracellularly, the receptor sits in the membrane of its neuron, usually localized at a synapse, postsynaptically. However, some isoforms may be found extrasynaptically, the net effect is typically inhibitory, reducing the activity of the neuron. The GABAA channel opens quickly and thus contributes to the part of the inhibitory post-synaptic potential. The endogenous ligand that binds to the site is inosine. There are numerous subunit isoforms for the GABAA receptor, which determine the receptors agonist affinity, chance of opening, conductance, five subunits can combine in different ways to form GABAA channels. The minimal requirement to produce a GABA-gated ion channel is the inclusion of both α and β subunits, but the most common type in the brain is a pentamer comprising two αs, two βs, and a γ. The receptor binds two GABA molecules, at the interface between an α and a β subunit, a number of ligands have been found to bind to various sites on the GABAA receptor complex and modulate it besides GABA itself
7.
Pharmacokinetics
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Pharmacokinetics, sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered to a living organism. The substances of interest include any chemical xenobiotic such as, pharmaceutical drugs, pesticides, food additives, cosmetic ingredients, etc. It attempts to analyze chemical metabolism and to discover the fate of a chemical from the moment that it is administered up to the point at which it is eliminated from the body. Pharmacokinetics is the study of how an organism affects a drug, both together influence dosing, benefit, and adverse effects, as seen in PK/PD models. Pharmacokinetic properties of chemicals are affected by the route of administration and these may affect the absorption rate. Models have been developed to simplify conceptualization of the processes that take place in the interaction between an organism and a chemical substance. The various compartments that the model is divided into are commonly referred to as the ADME scheme, absorption - the process of a substance entering the blood circulation. Distribution - the dispersion or dissemination of substances throughout the fluids, metabolism – the recognition by the organism that a foreign substance is present and the irreversible transformation of parent compounds into daughter metabolites. Excretion - the removal of the substances from the body, in rare cases, some drugs irreversibly accumulate in body tissue. The two phases of metabolism and excretion can also be grouped together under the title elimination, the study of these distinct phases involves the use and manipulation of basic concepts in order to understand the process dynamics. All these concepts can be represented through mathematical formulas that have a graphical representation. The model outputs for a drug can be used in industry or in the application of pharmacokinetic concepts. Clinical pharmacokinetics provides many performance guidelines for effective and efficient use of drugs for human-health professionals, in practice, it is generally considered that steady state is reached when a time of 4 to 5 times the half-life for a drug after regular dosing is started. Noncompartmental methods estimate the exposure to a drug by estimating the area under the curve of a concentration-time graph, compartmental methods estimate the concentration-time graph using kinetic models. Noncompartmental methods are more versatile in that they do not assume any specific compartmental model. The final outcome of the transformations that a drug undergoes in an organism, a number of functional models have been developed in order to simplify the study of pharmacokinetics. These models are based on a consideration of an organism as a number of related compartments, the simplest idea is to think of an organism as only one homogenous compartment. However, these models do not always reflect the real situation within an organism
8.
PubMed Identifier
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PubMed is a free search engine accessing primarily the MEDLINE database of references and abstracts on life sciences and biomedical topics. The United States National Library of Medicine at the National Institutes of Health maintains the database as part of the Entrez system of information retrieval, from 1971 to 1997, MEDLINE online access to the MEDLARS Online computerized database primarily had been through institutional facilities, such as university libraries. PubMed, first released in January 1996, ushered in the era of private, free, home-, the PubMed system was offered free to the public in June 1997, when MEDLINE searches via the Web were demonstrated, in a ceremony, by Vice President Al Gore. Information about the journals indexed in MEDLINE, and available through PubMed, is found in the NLM Catalog. As of 5 January 2017, PubMed has more than 26.8 million records going back to 1966, selectively to the year 1865, and very selectively to 1809, about 500,000 new records are added each year. As of the date,13.1 million of PubMeds records are listed with their abstracts. In 2016, NLM changed the system so that publishers will be able to directly correct typos. Simple searches on PubMed can be carried out by entering key aspects of a subject into PubMeds search window, when a journal article is indexed, numerous article parameters are extracted and stored as structured information. Such parameters are, Article Type, Secondary identifiers, Language, publication type parameter enables many special features. As these clinical girish can generate small sets of robust studies with considerable precision, since July 2005, the MEDLINE article indexing process extracts important identifiers from the article abstract and puts those in a field called Secondary Identifier. The secondary identifier field is to store numbers to various databases of molecular sequence data, gene expression or chemical compounds. For clinical trials, PubMed extracts trial IDs for the two largest trial registries, ClinicalTrials. gov and the International Standard Randomized Controlled Trial Number Register, a reference which is judged particularly relevant can be marked and related articles can be identified. If relevant, several studies can be selected and related articles to all of them can be generated using the Find related data option, the related articles are then listed in order of relatedness. To create these lists of related articles, PubMed compares words from the title and abstract of each citation, as well as the MeSH headings assigned, using a powerful word-weighted algorithm. The related articles function has been judged to be so precise that some researchers suggest it can be used instead of a full search, a strong feature of PubMed is its ability to automatically link to MeSH terms and subheadings. Examples would be, bad breath links to halitosis, heart attack to myocardial infarction, where appropriate, these MeSH terms are automatically expanded, that is, include more specific terms. Terms like nursing are automatically linked to Nursing or Nursing and this important feature makes PubMed searches automatically more sensitive and avoids false-negative hits by compensating for the diversity of medical terminology. The My NCBI area can be accessed from any computer with web-access, an earlier version of My NCBI was called PubMed Cubby
9.
Hypnotic
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This group is related to sedatives. Whereas the term sedative describes drugs that serve to calm or relieve anxiety, because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects they are often referred to collectively as sedative-hypnotic drugs. Hypnotic drugs are prescribed for insomnia and other sleep disorders. When prescribed, hypnotic medication should be used for the shortest period of time necessary, most hypnotics prescribed today are either benzodiazepines or nonbenzodiazepines. Among individuals with sleep disorders,13. 7% are taking or prescribed nonbenzodiazepines, while 10. 8% are taking benzodiazepines, early classes of drugs, such as barbiturates, have fallen out of use in most practices but are still prescribed for some patients. In children, prescribing hypnotics is not yet acceptable unless used to treat night terrors or somnambulism, falling outside of the above-mentioned categories, the neuro-hormone melatonin has a hypnotic function. Research about using medications to treat insomnia evolved throughout the last half of the 20th century, treatment for insomnia in psychiatry dates back to 1869 when chloral hydrate was first used as a soporific. Barbiturates emerged as the first class of drugs that emerged in the early 1900s, although the best drug family at the time they were dangerous in overdose. During the 1970s, quinazolinones and benzodiazepines were introduced as alternatives to replace barbiturates. Benzodiazepines are not without their drawbacks, substance dependence is possible, questions have been raised as to whether they disturb sleep architecture. Nonbenzodiazepines are the most recent development, although its clear that they are less toxic than their predecessors, barbiturates, comparative efficacy over benzodiazepines have not been established. Without longitudinal studies, it is hard to determine, however some psychiatrists recommend these drugs, other sleep remedies that may be considered sedative-hypnotics exist, psychiatrists will sometimes prescribe medicines off-label if they have sedating effects. Examples of these include mirtazapine, clonidine, quetiapine, and the over-the-counter sleep aid diphenhydramine, off-label sleep remedies are particularly useful when first-line treatment is unsuccessful or deemed unsafe. Barbiturates are drugs that act as central nervous system depressants, and can produce a wide spectrum of effects. They are also effective as anxiolytics, hypnotics, and anticonvulsants, barbiturates also have analgesic effects, however, these effects are somewhat weak, preventing barbiturates from being used in surgery in the absence of other analgesics. They have dependence liability, both physical and psychological, however, barbiturates are still used in general anesthesia, for epilepsy, and assisted suicide. Barbiturates are derivatives of barbituric acid, the principal mechanism of action of barbiturates is believed to be positive allosteric modulation of GABAA receptors. Examples include amobarbital, pentobarbital, phenobarbital, secobarbital, and sodium thiopental, quinazolinones are also a class of drugs which function as hypnotic/sedatives that contain a 4-quinazolinone core
10.
Alcohol
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In chemistry, an alcohol is any organic compound in which the hydroxyl functional group is bound to a saturated carbon atom. The term alcohol originally referred to the alcohol ethanol, the predominant alcohol in alcoholic beverages. The suffix -ol in non-systematic names also typically indicates that the substance includes a functional group and, so. But many substances, particularly sugars contain hydroxyl functional groups without using the suffix, an important class of alcohols, of which methanol and ethanol are the simplest members is the saturated straight chain alcohols, the general formula for which is CnH2n+1OH. The word alcohol is from the Arabic kohl, a used as an eyeliner. Al- is the Arabic definite article, equivalent to the in English, alcohol was originally used for the very fine powder produced by the sublimation of the natural mineral stibnite to form antimony trisulfide Sb 2S3, hence the essence or spirit of this substance. It was used as an antiseptic, eyeliner, and cosmetic, the meaning of alcohol was extended to distilled substances in general, and then narrowed to ethanol, when spirits as a synonym for hard liquor. Bartholomew Traheron, in his 1543 translation of John of Vigo, Vigo wrote, the barbarous auctours use alcohol, or alcofoll, for moost fine poudre. The 1657 Lexicon Chymicum, by William Johnson glosses the word as antimonium sive stibium, by extension, the word came to refer to any fluid obtained by distillation, including alcohol of wine, the distilled essence of wine. Libavius in Alchymia refers to vini alcohol vel vinum alcalisatum, Johnson glosses alcohol vini as quando omnis superfluitas vini a vino separatur, ita ut accensum ardeat donec totum consumatur, nihilque fæcum aut phlegmatis in fundo remaneat. The words meaning became restricted to spirit of wine in the 18th century and was extended to the class of substances so-called as alcohols in modern chemistry after 1850, the term ethanol was invented 1892, based on combining the word ethane with ol the last part of alcohol. In the IUPAC system, in naming simple alcohols, the name of the alkane chain loses the terminal e and adds ol, e. g. as in methanol and ethanol. When necessary, the position of the group is indicated by a number between the alkane name and the ol, propan-1-ol for CH 3CH 2CH 2OH, propan-2-ol for CH 3CHCH3. If a higher priority group is present, then the prefix hydroxy is used, in other less formal contexts, an alcohol is often called with the name of the corresponding alkyl group followed by the word alcohol, e. g. methyl alcohol, ethyl alcohol. Propyl alcohol may be n-propyl alcohol or isopropyl alcohol, depending on whether the group is bonded to the end or middle carbon on the straight propane chain. As described under systematic naming, if another group on the molecule takes priority, Alcohols are then classified into primary, secondary, and tertiary, based upon the number of carbon atoms connected to the carbon atom that bears the hydroxyl functional group. The primary alcohols have general formulas RCH2OH, the simplest primary alcohol is methanol, for which R=H, and the next is ethanol, for which R=CH3, the methyl group. Secondary alcohols are those of the form RRCHOH, the simplest of which is 2-propanol, for the tertiary alcohols the general form is RRRCOH
11.
Alcohol (drug)
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Ethanol, also called alcohol, ethyl alcohol, and drinking alcohol, is the principal type of alcohol found in alcoholic beverages. It is a volatile, flammable, colorless liquid with a characteristic odor. Its chemical formula is C 2H 6O, which can be written also as CH 3-CH 2-OH or C 2H 5-OH, ethanol is mostly produced by the fermentation of sugars by yeasts, or by petrochemical processes. It is a psychoactive drug, causing a characteristic intoxication. It is widely used as a solvent, as fuel, and as a feedstock for synthesis of other chemicals, the eth- prefix and the qualifier ethyl in ethyl alcohol originally come from the name ethyl assigned in 1834 to the group C 2H 5- by Justus Liebig. He coined the word from the German name Aether of the compound C 2H 5-O-C 2H5, according to the Oxford English Dictionary, Ethyl is a contraction of the Ancient Greek αἰθήρ and the Greek word ύλη. The name ethanol was coined as a result of a resolution that was adopted at the International Conference on Chemical Nomenclature that was held in April 1892 in Geneva, Switzerland. The term alcohol now refers to a class of substances in chemistry nomenclature. The Oxford English Dictionary claims that it is a loan from Arabic al-kuḥl, a powdered ore of antimony used since aniquity as a cosmetic. The use of alcohol for ethanol is modern, first recorded 1753, the systematic use in chemistry dates to 1850. Ethanol is used in medical wipes and most common antibacterial hand sanitizer gels as an antiseptic, ethanol kills organisms by denaturing their proteins and dissolving their lipids and is effective against most bacteria and fungi, and many viruses. However, ethanol is ineffective against bacterial spores, ethanol may be administered as an antidote to methanol and ethylene glycol poisoning. Ethanol, often in high concentrations, is used to dissolve many water-insoluble medications, as a central nervous system depressant, ethanol is one of the most commonly consumed psychoactive drugs. The amount of ethanol in the body is typically quantified by blood alcohol content, small doses of ethanol, in general, produce euphoria and relaxation, people experiencing these symptoms tend to become talkative and less inhibited, and may exhibit poor judgment. Ethanol is commonly consumed as a drug, especially while socializing. The largest single use of ethanol is as a fuel and fuel additive. Brazil in particular relies heavily upon the use of ethanol as an engine fuel, gasoline sold in Brazil contains at least 25% anhydrous ethanol. Hydrous ethanol can be used as fuel in more than 90% of new gasoline fueled cars sold in the country, Brazilian ethanol is produced from sugar cane and noted for high carbon sequestration
12.
Ethchlorvynol
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Ethchlorvynol/ˌɛθklɔːrˈvaɪnɒl/ is a sedative and hypnotic medication developed by Pfizer in the 1950s. In the United States it was sold by Abbott Laboratories under the tradename Placidyl, Placidyl was available in 200 mg.500 mg. and 750 mg. strength capsules. While the 500 mg. and 750 mg. strength capsules were for use in reducing sleep latency, Abbott discontinued production in 1999, after which Placidyl was available for about a year in the United States. Although, theoretically, ethchlorvynol could be manufactured for sale in the United States by another pharmaceutical company, individuals with a valid prescription for the substance may legally transport a reasonable amount of ethclorvynol with them into the United States. Ethchlorvynol was used to treat insomnia, but prescriptions for the drug had fallen significantly by 1990, as other hypnotics that were considered safer became much more common. It is no longer prescribed in the United States due to unavailability, along with expected sedative effects of relaxation and drowsiness, adverse reactions to ethchlorvynol include skin rash, faintness, restlessness and euphoria. Early adjustment side effects may include nausea and vomiting, numbness, blurred vision, stomach pains, after prolonged use, withdrawal symptoms may include convulsions, hallucinations, and amnesia. As with most hypnotics, Placidyl was indicated for use in the treatment of insomnia for a period of time. However, it was not uncommon for doctors to prescribe Placidyl for extended periods of time. During the late 1970s, ethchlorvynol was sometimes over-prescribed causing an epidemic of persons who quickly became addicted to this powerful drug. Occasional deaths would occur when addicted persons would try to inject the drug directly into a vein or an artery, ethchlorvynol is not compatible with intravenous injection and serious injury or death can occur when it is used in this manner. Ethchlorvynol is a member of the class of sedative-hypnotic carbinols, which includes methylparafynol and it is not a barbituric acid derivative. The systematic name of ethchlorvynol is usually given as ethyl 2-chlorovinyl ethynyl carbinol or 1-chloro-3-ethylpent-1-en-4-yn-3-ol, ethchlorvynol is synthesized by an ethynylation reaction using lithium acetylide and 1-chloro-1-penten-3-one in liquid ammonia, followed by acidic work-up. Electronic Orange Book, Approved Drug Products with Therapeutic Equivalence Evaluations Food and Drug Administration
13.
2,2,2-Trichloroethanol
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2,2, 2-Trichloroethanol is an organic compound related to ethanol, except the hydrogen atoms at position 2 are replaced with chlorine atoms. In humans, its effects are similar to those of its prodrugs, chloral hydrate. It has, historically, been used as a sedative hypnotic, the hypnotic drug triclofos is metabolized in vivo to 2,2, 2-trichloroethanol. Chronic exposure may result in kidney and liver damage
14.
Barbiturate
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A barbiturate is a drug that acts as a central nervous system depressant, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, hypnotics, and anticonvulsants and these effects, however, are somewhat weak, and may react with a patients other medications or sedatives. This fact precludes barbiturates from being used in surgery or in the presence of other analgesics, in mice, barbiturates are hyperalgesic, increasing the sensitivity to pain. Barbiturates have addiction potential, both physical and psychological, Barbiturates are derivatives of barbituric acid. However, barbiturates are still used as anticonvulsants, as para-operative sedatives, Barbiturates in high doses are used for physician-assisted suicide, and in combination with a muscle relaxant for euthanasia and for capital punishment by lethal injection. Barbiturates are frequently employed as euthanizing agents in veterinary medicine. Thiopental is a barbiturate that is marketed under the name sodium pentothal. When dissolved in water, sodium amytal can be swallowed, or it can be administered by intravenous injection, the memory-impairing effects and cognitive impairments induced by the drug are thought to reduce a subjects ability to invent and remember lies. There are special risks to consider for older adults, women who are pregnant, when a person ages, the body becomes less able to rid itself of barbiturates. As a result, people over the age of sixty-five are at risk of experiencing the harmful effects of barbiturates, including drug dependence. When barbiturates are taken during pregnancy, the passes through the mothers gastric juice to her fetus. After the baby is born, it may experience withdrawal symptoms and have trouble breathing, in addition, nursing mothers who take barbiturates may transmit the drug to their babies through breast milk. A rare adverse reaction to barbiturates is Stevens-Johnson syndrome, which affects the mucous membranes. With regular use, tolerance to the effects of barbiturates develops, similar to benzodiazepines the longer acting barbiturates produce a less severe withdrawal syndrome than short acting and ultra short acting barbiturates. Withdrawal symptoms are dose-dependent with heavier users being affected worse than lower-dose addicts, mental cravings for barbiturates can last for months or years in some cases and counselling/support groups are highly encouraged by addiction specialists. The lethal dosage of barbiturates varies greatly with tolerance and from one individual to another, tolerance to the anticonvulsant effects tends to correlate more with tolerance to physiological effects, however, meaning that they are still a viable option for long-term epilepsy treatment. Barbiturates in overdose with other CNS depressants are even more due to additive CNS. The longest-acting barbiturates have half-lives of a day or more, Barbiturates induce a number of hepatic CYP enzymes, leading to exaggerated effects from many prodrugs and decreased effects from drugs which are metabolized by these enzymes to inactive metabolites
15.
Amobarbital
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Amobarbital is a drug that is a barbiturate derivative. It is a crystalline powder with no odor and a slightly bitter taste. It was first synthesized in Germany in 1923, if amobarbital is taken for extended periods of time, physical and psychological dependence can develop. Amobarbital withdrawal mimics delirium tremens and may be life-threatening, Amobarbital has been used in a study to inhibit mitochondrial electron transport in the rat heart. A1988 study found that amobarbital increases benzodiazepine receptor binding in vivo with less potency than secobarbital and pentobarbital and it has an LD50 in mice of 212 mg/kg s. c. Amobarbital undergoes both hydroxylation to form 3-hydroxyamobarbital, and N-glucosidation to form 1-amobarbital, anxiety Epilepsy Insomnia Wada test When given slowly by an intravenous route, sodium amobarbital has a reputation for acting as a so-called truth serum. Under the influence, a person will divulge information that under normal circumstances they would block, as such, the drug was first employed clinically by Dr. William Bleckwenn at the University of Wisconsin to circumvent inhibitions in psychiatric patients. The use of amobarbital as a truth serum has lost credibility due to the discovery that a subject can be coerced into having a memory of the event. The drug may be used intravenously to interview patients with catatonic mutism and it was used by the United States armed forces during World War II in an attempt to treat shell shock and return soldiers to the front-line duties. This use has since been discontinued as the powerful sedation, cognitive impairment, being chemically related to phenobarbital, it might also do the same thing to digitoxin, a cardiac glycoside. Amobarbital, like all barbiturates, is synthesized by reacting malonic acid derivatives with urea derivatives, in particular, in order to make amobarbital, α-ethyl-α-isoamylmalonic ester is reacted with urea. It has been used to convict alleged murderers such as Andres English-Howard and he was surreptitiously administered the drug by his lawyer, and under the influence of it he revealed why he strangled her and under what circumstances. A year later he confessed on the stand and was convicted on the basis of these statements. He later committed suicide in his cell, on the night of August 28,1951, Robert Walkers housekeeper found the actor in an emotional state. She called Walkers psychiatrist who arrived and administered amobarbital for sedation, walker was allegedly drinking prior to his emotional outburst, and it is believed the combination of amobarbital and alcohol resulted in a severe reaction. As a result, he passed out and stopped breathing, walker died at 32 years old. Street names for Amobarbital include blues, blue angles, blue birds, and blue devils
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Hexobarbital
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Hexobarbital or hexobarbitone, sold both in acid and sodium salt forms as Citopan, Evipan, and Tobinal, is a barbiturate derivative having hypnotic and sedative effects. It was also used to women prisoners at Ravensbruck Concentration Camp. Modern barbiturates has largely supplanted the use of hexobarbital as an anesthetic, hexobarbital is still used in some scientific research. Hexobarbital is a white powder with a bitter taste. It melts at 146.5 °C and has a constant of 8.2. New aspects of hexobarbital metabolism, Stereoselective metabolism, new metabolic pathway via GSH conjugation, a study of the duration of acute tolerance induced with hexobarbital in male rats. Korkmaz, S. Ljungblad, E. Wahlström, G. Interaction between flumazenil and the effects of hexobarbital in the rat. Schmidt, A. Nordholm, L. Interaction of the competitive AMPA receptor antagonist NBQX with hexobarbital
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Methohexital
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Methohexital or methohexitone is a drug which is a barbiturate derivative. It is classified as short-acting, and has an onset of action. It is similar in its effects to sodium thiopental, a drug with which it competed in the market for anaesthetics, Methohexital binds to a distinct site which is associated with Cl− ionophores at GABAA receptors. This increases the length of time which the Cl− ionopores are open, metabolism of methohexital is primarily hepatic via demethylation and oxidation. Side-chain oxidation is the means of metabolism involved in the termination of the drugs biological activity. Protein binding is approximately 73% for methohexital, Methohexital is primarily used to induce anesthesia, and is generally provided as a sodium salt. It is only used in hospital or similar settings, under strict supervision and it has been commonly used to induce deep sedation or general anesthesia for surgery and dental procedures. Unlike many other barbiturates, Methohexital actually lowers the seizure threshold, and rapid recovery rate with consciousness being gained within three to seven minutes after induction and full recovery within 30 minutes is a major advantage over other ECT barbiturates. The resulting allyl- malonic ester is synthesized by subsequent alkylation of the malonic ester itself, beginning with 2-bromo-3-hexyne, which gives malonic ester, in the final step, reaction of the disubstituted malonic ester with N-methylurea gives desired methohexital. RxList. com - Methohexital Drugs. com - Methohexital Sodium DrugLib. com - Brevital
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Talbutal
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Talbutal is a barbiturate with a short to intermediate duration of action. It is an isomer of butalbital. Talbutal is a schedule III drug in the U. S. Talbutal is a short to intermediate-acting barbiturate, barbiturates act as nonselective depressants of the central nervous system, capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high doses, barbiturates induce anesthesia. Talbutal binds at a binding site associated with a Cl− ionopore at the GABAA receptor. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, symptoms of acute barbiturate poisoning include drowsiness, confusion, coma, respiratory depression, hypotension, and shock
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Sodium thiopental
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Sodium thiopental, also known as Sodium Pentothal, thiopental, thiopentone, or Trapanal, is a rapid-onset short-acting barbiturate general anesthetic that is an analogue of thiobarbital. Sodium thiopental was a medicine in the World Health Organizations Essential Drugs List, which is a list of minimum medical needs for a basic healthcare system. Sodium thiopental is an ultra-short-acting barbiturate and has been used commonly in the phase of general anesthesia. Its use has largely replaced with that of propofol, but retains popularity as an induction agent for rapid sequence intubation. Following intravenous injection, the drug reaches the brain and causes unconsciousness within 30–45 seconds. At one minute, the drug attains a peak concentration of about 60% of the dose in the brain. Thereafter, the drug distributes to the rest of the body, a normal dose of sodium thiopental given to a pregnant woman for operative delivery rapidly makes her unconscious, but the baby in her uterus remains conscious. However, larger or repeated doses can depress the baby, instead, anesthesia is usually maintained with an inhaled anesthetic agent. Inhaled anesthetics are eliminated quickly, so that stopping the inhaled anesthetic will allow rapid return of consciousness. Sodium thiopental would have to be given in large amounts to maintain an anesthetic plane, in veterinary medicine, sodium thiopental is used to induce anesthesia in animals. Since it is redistributed to fat, certain breeds of dogs such as sight hounds will have prolonged recoveries from sodium thiopental due to their lack of body fat. Conversely, obese animals will have rapid recoveries, but it will be some time before it is removed from their bodies. Sodium thiopental is always administered intravenously, as it can be irritating, severe tissue necrosis. Sodium thiopental decreases the stroke volume, which results in a decrease in cardiac output. The decrease in cardiac output occurs in conjunction with a decrease in vascular resistance. However, in comparison with propofol, the reflex tachycardia seen during states of hypotension is relatively spared, in addition to anesthesia induction, sodium thiopental was historically used to induce medical comas. It has now superseded by drugs such as propofol because their effects wear off more quickly than thiopental. Patients with brain swelling, causing elevation of pressure, either secondary to trauma or following surgery
