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2β-Propanoyl-3β-(2-naphthyl)-tropane
2β-Propanoyl-3β-(2-naphthyl)-tropane or WF-23 (Wake Forest-23, named after the university where it was first created) is a cocaine analogue. It is several hundred times more potent than cocaine at being a serotonin-norepinephrine-dopamine reuptake inhibitor. As can be seen on PubMed, these acyl substituted phenyltropanes are highly potent MAT inhibitors and also have a very long half-life, spanning perhaps at least a few days; as the half-life of the dopamine transporter in rats was found to be 2-3 days under normal conditions (with agonists, antagonists, and transporter inhibitors altering the half-life), it may be that WF-23 largely or mostly binds to its transporters until they are degraded. See also * HDEP-28 * HDMP-28 * List of cocaine analogues This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemical compound from (often the starting point of natural) cocaine's molecular structure, with the result product suf ...
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HDEP-28
HDEP-28 or ethylnaphthidate is a piperidine based stimulant drug, closely related to ethylphenidate, but with the benzene ring replaced by naphthalene. It is even more closely related to HDMP-28, which acts as a potent serotonin–norepinephrine–dopamine reuptake inhibitor with several times the potency of methylphenidate and a short duration of action. Legality HDEP-28 was banned in the UK as a Temporary Class Drug from June 2015 following its unapproved sale as a designer drug, alongside 4-Methylmethylphenidate. See also * 2β-Propanoyl-3β-(2-naphthyl)-tropane (WF-23) * 3,4-Dichloromethylphenidate * 4-Methylmethylphenidate * 4-Fluoromethylphenidate * Isopropylphenidate * Naphthylisopropylamine * Naphyrone * Propylphenidate Propylphenidate (also known as PPH) is a piperidine based stimulant drug, closely related to methylphenidate, but with the methyl ester replaced by a propyl ester. It was banned in the UK as a Temporary Class Drug from April 2015 following its u ...
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HDMP-28
HDMP-28 or methylnaphthidate is a piperidine based stimulant drug, closely related to methylphenidate, but with the benzene ring replaced by naphthalene. It is a potent dopamine reuptake inhibitor, with several times the potency of methylphenidate and a short duration of action, and is a structural isomer of another potent dopamine reuptake inhibitor, N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate. Most of the TMP analogs of HDMP-28 have SERT Ki values in the range >10,000 and so are selective for dopamine and noradrenaline reuptake, with little or no effect on serotonin. HDMP-28 has high affinity to SERT, and so behaves as a triple reuptake inhibitor. D.R. = Discrimination Ratio = HA ÷ HFT. A low D.R. = addictive, whereas a high D.R. = low propensity for self-administration. Legality HDMP-28 is illegal in Switzerland as of December 2015. See also * 3-Bromomethylphenidate * 3,4-Dichloromethylphenidate * BMAPN * Ethylphenidate * HDEP-28 * Naphthylisopropyla ...
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Cocaine
Cocaine (from , from , ultimately from Quechuan languages, Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly recreational drug use, used recreationally for its euphoria, euphoric effects. It is primarily obtained from the leaves of two Coca species native to South America, ''Erythroxylum coca'' and ''Erythroxylum novogranatense''. After extraction from coca leaves and further processing into cocaine hydrochloride (powdered cocaine), the drug is often Insufflation (medicine), snorted, applied topical administration, topically to the mouth, or dissolved and injection (medicine), injected into a vein. It can also then be turned into free base form (crack cocaine), in which it can be heated until sublimated and then the vapours can be smoking, inhaled. Cocaine stimulates the mesolimbic pathway, reward pathway in the brain. Mental effects may include an euphoria, intense feeling of happiness, sexual arousal, psychosis, loss of contact with reality, or psychomo ...
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Analog (chemistry)
A structural analog (analogue in modern traditional English; Commonwealth English), also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is screened for structural analogs of a lead compound. Chemical analogues of il ...
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PubMed
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 (NLM) at the National Institutes of Health maintain the database as part of the Entrez system of information retrieval. From 1971 to 1997, online access to the MEDLINE database had been primarily through institutional facilities, such as university libraries. PubMed, first released in January 1996, ushered in the era of private, free, home- and office-based MEDLINE searching. The PubMed system was offered free to the public starting in June 1997. Content In addition to MEDLINE, PubMed provides access to: * older references from the print version of ''Index Medicus'', back to 1951 and earlier * references to some journals before they were indexed in Index Medicus and MEDLINE, for instance ''Science'', ''BMJ'', and ''Annals of Surgery'' * very recent entries to records for an article before it ...
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Monoamine Transporter
Monoamine transporters (MATs) are protein structures that function as integral plasma-membrane transporters to regulate concentrations of extracellular monoamine neurotransmitters. Three major classes of MATs (SERT, DAT, NET) are responsible for the reuptake of their associated amine neurotransmitters (serotonin, dopamine, norepinephrine). MATs are located just outside the synaptic cleft (peri-synaptically), transporting monoamine transmitter overflow from the synaptic cleft back to the cytoplasm of the pre-synaptic neuron. MAT regulation generally occurs through protein phosphorylation and posttranslational modification. Due to their significance in neuronal signaling, MATs are commonly associated with drugs used to treat mental disorders as well as recreational drugs. Compounds targeting MATs range from medications such as the wide variety of tricyclic antidepressants, selective serotonin reuptake inhibitors such as fluoxetine (Prozac) to stimulant medications such as methylp ...
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Half-life
Half-life (symbol ) is the time required for a quantity (of substance) to reduce to half of its initial value. The term is commonly used in nuclear physics to describe how quickly unstable atoms undergo radioactive decay or how long stable atoms survive. The term is also used more generally to characterize any type of exponential (or, rarely, non-exponential) decay. For example, the medical sciences refer to the biological half-life of drugs and other chemicals in the human body. The converse of half-life (in exponential growth) is doubling time. The original term, ''half-life period'', dating to Ernest Rutherford's discovery of the principle in 1907, was shortened to ''half-life'' in the early 1950s. Rutherford applied the principle of a radioactive element's half-life in studies of age determination of rocks by measuring the decay period of radium to lead-206. Half-life is constant over the lifetime of an exponentially decaying quantity, and it is a characteristic unit for ...
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List Of Cocaine Analogues
This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemical compound from (often the starting point of natural) cocaine's molecular structure, with the result product sufficiently similar to cocaine to display similarity in, but alteration to, its chemical function. Within the scope of analogous compounds created from the structure of cocaine, so named "cocaine analogues" retain 3''β''-benzoyloxy or similar functionality (the term specifically used usually distinguishes from phenyltropanes, but in the broad sense generally, as a category, includes them) on a tropane skeleton, as compared to other stimulants of the kind. Many of the semi-synthetic cocaine analogues ''proper'' which have been made & studied have consisted of among the nine following classes of compounds: * stereoisomers of cocaine * 3''β''-phenyl ring substituted analogues * 2''β''-substituted analogues * ''N''-modified analogues of cocaine * 3''β''-carbamoyl a ...
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Tropanes
Tropane alkaloids are a class of bicyclic .2.1alkaloids and secondary metabolites that contain a tropane ring in their chemical structure. Tropane alkaloids occur naturally in many members of the plant family Solanaceae. Certain tropane alkaloids such as cocaine and scopolamine are notorious for their psychoactive effects, related usage and cultural associations. Particular tropane alkaloids such as these have pharmacological properties and can act as anticholinergics or stimulants. Classification Anticholinergics Anticholinergic drugs and deliriants: * Atropine, racemic hyoscyamine, from the deadly nightshade (''Atropa belladonna'') * Hyoscyamine, the ''levo''-isomer of atropine, from henbane (''Hyoscyamus niger''), mandrake (''Mandragora officinarum'') and the sorcerers' tree (''Latua pubiflora''). * Scopolamine, from henbane and ''Datura'' species (Jimson weed) All three acetylcholine-inhibiting chemicals can also be found in the leaves, stems, and flowers in varying, un ...
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Stimulants
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have Sympathomimetic drug, sympathomimetic effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or Prohibition (drugs), illicitly) as performance-enhancing substance, performance-enhancing or recreational drug use, recreational drugs. Among narcotics, stimulants produce a noticeable crash or ''Comedown (drugs), comedown'' at the end of their effects. The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall). It was estimated in 2015 that the percentage of the world population that had used cocaine during a year was 0.4%. For the category "amphetamines and p ...
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