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Mecamylamine
Mecamylamine (INN, BAN; or mecamylamine hydrochloride (USAN); brand names Inversine, Vecamyl) is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors (nAChRs) that was introduced in the 1950s as an antihypertensive drug. In the United States, it was voluntarily withdrawn from the market in 2009 but was brought to market in 2013 as Vecamyl and eventually was marketed by Turing Pharmaceuticals. Chemically, mecamylamine is a secondary aliphatic amine, with a pKaH of 11.2 Medical uses Mecamylamine has been used as an orally-active ganglionic blocker in treating autonomic dysreflexia and hypertension, but, like most ganglionic blockers, it is more often used now as a research tool. Mecamylamine is also sometimes used as an antiaddictive drug to help people stop smoking tobacco, and is now more widely used for this application than it is for lowering blood pressure. This effect is thought to be due to its blocking α3β4 nicotinic receptors in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-3 Beta-4 Nicotinic Receptor
The alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor and the ganglion-type nicotinic receptor,Pharmacology, (Rang, Dale, Ritter & Moore, , 5th ed., Churchill Livingstone 2003) p. 138. is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits. It is located in the autonomic ganglia and adrenal medulla, where activation yields post- and/or presynaptic excitation, mainly by increased Na+ and K+ permeability. As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric α3)m(β4)n where m + n = 5 The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries. Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, making α3β4 a promising target for the development of novel antiaddictive agents. Ligands Source: Agonists * Acetylcholine (endogenous neurotransmitter that b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-4 Beta-2
The alpha-4 beta-2 nicotinic receptor, also known as the α4β2 receptor, is a type of nicotinic acetylcholine receptor implicated in learning, consisting of α4 and β2 subunits. It is located in the brain, where activation yields post- and presynaptic excitation, mainly by increased Na+ and K+ permeability. Stimulation of this receptor subtype is also associated with growth hormone secretion. People with the inactive CHRNA4 mutation Ser248Phe are an average of 10 cm (4 inches) shorter than average and predisposed to obesity. A 2015 review noted that stimulation of the α4β2 nicotinic receptor in the brain is responsible for certain improvements in attentional performance; among the nicotinic receptor subtypes, nicotine has the highest binding affinity at the α4β2 receptor (ki=1 ), which is also the primary biological target that mediates nicotine's addictive properties. The receptors exist in the two stoichiometries: *(α4)2(β2)3 receptors have high sensiti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiaddictive
Addiction is a neuropsychological disorder characterized by a persistent and intense urge to use a drug or engage in a behavior that produces natural reward, despite substantial harm and other negative consequences. Repetitive drug use can alter brain function in synapses similar to natural rewards like food or falling in love in ways that perpetuate craving and weakens self-control for people with pre-existing vulnerabilities. This phenomenon – drugs reshaping brain function – has led to an understanding of addiction as a brain disorder with a complex variety of psychosocial as well as neurobiological factors that are implicated in the development of addiction. While mice given cocaine showed the compulsive and involuntary nature of addiction, for humans this is more complex, related to behavior or personality traits. Classic signs of addiction include compulsive engagement in rewarding stimuli, ''preoccupation'' with substances or behavior, and continued use despite n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Retrophin
Martin Shkreli (; born March 17, 1983) is an American investor, businessman and financial criminal. Shkreli is the co-founder of the hedge funds Elea Capital, MSMB Capital Management, and MSMB Healthcare, the co-founder and former CEO of pharmaceutical firms Retrophin and Turing Pharmaceuticals, and the former CEO of start-up software company Gödel Systems, which he founded in August 2016. In September 2015, Shkreli was widely criticized when Turing obtained the manufacturing license for the antiparasitic drug Daraprim and raised its price to insurance companies from $13.50 to $750.00 (USD) per pill. In 2017, Shkreli was convicted in federal court on two counts of securities fraud and one count of conspiracy. He was sentenced to seven years in prison and up to $7.4 million in fines. In the civil antitrust case, Shkreli was fined a further $64.6 million to be repaid to victims. In May2022, he was released early from the low-security federal prison in Allenwood, Pen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Layton Bioscience
Layton or The Laytons may refer to: Places United States * Layton, Florida, a city * Layton Township, Pottawattamie County, Iowa * Layton, New Jersey, an unincorporated community * Layton, Pennsylvania, an unincorporated community * Layton, Utah, a city England * Layton, Blackpool, a district of the town of Blackpool, Lancashire, England American schools * Layton High School, Layton, Utah * Layton School of Art, a former post-secondary school in Milwaukee, Wisconsin * Layton Preparatory School, a private preparatory school in Centreville, Delaware Transportation * Layton railway station (England), Layton, Lancashire * Layton station (FrontRunner), a commuter rail station in Layton, Utah * Layton Bridge, a road bridge (formerly a railroad bridge) in Pennsylvania, United States, on the National Register of Historic Places People * Layton (surname) * Layton (given name) Other uses * Baron Layton, a title in the Peerage of the United Kingdom * Professor Hershel Layton, title ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Merck & Co
Merck & Co., Inc. is an American Multinational corporation, multinational pharmaceutical company headquartered in Rahway, New Jersey. The company does business as Merck Sharp & Dohme or MSD outside the United States and Canada. It is one of the largest pharmaceutical companies in the world, generally ranking in the global top five by revenue. Merck & Co. was originally established as the American affiliate of Merck Group in 1891. Merck develops and produces medicines, vaccines, biologic therapies and animal health products. It has several blockbuster products, including cancer immunotherapy, anti-diabetic medications, and vaccines for HPV and chickenpox, each generating significant revenue as of 2020. The company is ranked 71st on the 2022 Fortune 500, ''Fortune'' 500 and 87th on the 2022 Forbes Global 2000, ''Forbes'' Global 2000, both based on 2021 revenues. In 2023, the company’s seat in the ''Forbes'' Global 2000 was 73. Products The company develops medicines, vaccines, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiomer
In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities which are mirror images of each other and non-superposable. Enantiomer molecules are like right and left hands: one cannot be superposed onto the other without first being converted to its mirror image. It is solely a relationship of chirality (chemistry), chirality and the permanent three-dimensional relationships among molecules or other chemical structures: no amount of re-orientation of a molecule as a whole or conformational isomerism, conformational change converts one chemical into its enantiomer. Chemical structures with chirality rotate plane-polarized light. A mixture of equal amounts of each enantiomer, a ''racemic mixture'' or a ''racemate'', does not rotate light. Stereoisomers include both enantiomers and diastereomers. Diaste ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dissociation Constant
In chemistry, biochemistry, and pharmacology, a dissociation constant (''K''D) is a specific type of equilibrium constant that measures the propensity of a larger object to separate (dissociate) reversibly into smaller components, as when a complex falls apart into its component molecules, or when a salt splits up into its component ions. The dissociation constant is the inverse of the association constant. In the special case of salts, the dissociation constant can also be called an ionization constant. For a general reaction: : A_\mathit B_\mathit \mathit A + \mathit B in which a complex \ce_x \ce_y breaks down into ''x'' A subunits and ''y'' B subunits, the dissociation constant is defined as : K_\mathrm = \frac where and ''x'' B''y''are the equilibrium concentrations of A, B, and the complex A''x'' B''y'', respectively. One reason for the popularity of the dissociation constant in biochemistry and pharmacology is that in the frequen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
