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5-ht2b
5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the ''HTR2B'' gene. 5-HT2B is a member of the 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Tissue distribution and function First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of hallucinogenic substituted amphetamines. The 5-HT2B receptor is expressed in several areas of the CNS, including the dorsal hypothalamus, frontal cortex, medi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BW-723C86
BW-723C86 is a tryptamine derivative drug which acts as a 5-HT2B receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues. BW-723C86 is actually a mixed 5-HT2B/5-HT2C agonist, and while it has good selectivity over 5-HT2A and other serotonin receptor subtypes, it is around only 3 times as selective for 2B compared to 2C and so is much less selective than most research ligands, but no superior 5-HT2B agonist was available until the potent and selective 5-HT2B activity of 6-APB was discovered in 2012. Highly selective 5-HT2C antagonists are available however, and so a combination of BW-723C86 with a selective 5-HT2C antagonist allows 5-HT2B mediated responses to be studied in isolation. An in vitro study including assay on normal (healthy) human melanocytes found that BW-723C86 causes skin whitening. The mechanism of action of BW-723C86 is decreasing the expression of MITF w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, responding to stimuli, providing structure to cells and organisms, and transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the nucleotide sequence of their genes, and which usually results in protein folding into a specific 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called peptides. The individual amino acid residues are bonded together by peptide bonds and adjacent amino acid residues. The sequence of amino acid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and othe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aminorex
Aminorex (Menocil, Apiquel, aminoxaphen, aminoxafen, McN-742) is a weight loss (anorectic) stimulant drug. It was withdrawn from the market after it was found to cause pulmonary hypertension. In the U.S., it is an illegal Schedule I drug, meaning it has high abuse potential, no accepted medical use, and a poor safety profile. Aminorex, in the 2-amino-5-aryl oxazoline class, was developed by McNeil Laboratories in 1962. It is closely related to 4-methylaminorex. Aminorex has been shown to have locomotor stimulant effects, lying midway between dextroamphetamine and methamphetamine. Aminorex effects have been attributed to the release of catecholamines. It can be produced as a metabolite of the worming medication levamisole, which is sometimes used as a cutting agent of illicitly produced cocaine. History It was discovered in 1962 by Edward John Hurlburt, and was quickly found in 1963 to have an anorectic effect in rats. It was introduced as a prescription appetite suppr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chlorphentermine
Chlorphentermine (trade names Apsedon, Desopimon, Lucofen) is a serotonergic appetite suppressant of the amphetamine family. Developed in 1962, it is the 4-chloro derivative of the better known appetite suppressant phentermine, which is still in current use. Chlorphentermine acts as a highly selective serotonin releasing agent (SRA). It is not a psychostimulant and has little or no abuse potential, but is classed as a Schedule III drug in the USA due mainly to its similarity to other appetite suppressants such as diethylpropion which have been more widely abused. It is no longer used due mainly to safety concerns, as it has a serotonergic effects profile similar to other withdrawn appetite suppressants such as fenfluramine and aminorex which were found to cause pulmonary hypertension and cardiac fibrosis following prolonged use. The plasma half-life is about five days. It was withdrawn from the market in the UK in 1974. See also * Aminorex * Cericlamine * Cloforex * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norfenfluramine
Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist. See also * Fenfluramine * Benfluorex * Norfenfluramine is the precursor to flucetorex Flucetorex (INN) is an amphetamine. It was investigated as an anorectic, but does not appear to have ever been marketed. It is related to fenfluramine. See also * Benfluorex * Fludorex * Tiflorex Tiflorex, formerly known a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cabergoline
Cabergoline, sold under the brand name Dostinex among others, is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson's disease, and for other indications. It is taken by mouth. Cabergoline is an ergot derivative and a potent dopamine D2 receptor agonist. Cabergoline was patented in 1980 and approved for medical use in 1993. Medical uses * Lactation suppression * HyperprolactinemiaUK electronic Medicines CompendiuDostinex TabletsLast Updated on eMC Dec 23, 2013 * Adjunctive therapy of prolactin-producing pituitary gland tumors ( prolactinomas); * Monotherapy of Parkinson's disease in the early phase; * Combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson's disease; * In some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, nonpuerperal mastitis and galactorrhea); * Treatment of uter ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pergolide
Pergolide, sold under the brand name Permax and Prascend (veterinary) among others, is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with reduced dopamine activity in the substantia nigra of the brain. Pergolide acts on many of the same receptors as dopamine to increase receptor activity. It was patented in 1978 and approved for medical use in 1989. In 2007, pergolide was withdrawn from the U.S. market for human use after several published studies revealed a link between the drug and increased rates of valvular heart disease. However, a veterinary form of pergolide, marketed under the trade name Prascend, is permitted for the treatment of pituitary pars intermedia dysfunction (PPID) also known as equine Cushing's syndrome (ECS) in horses. Medical uses Pergolide is not available for use by humans in the United States, however, it is still used in various other countries, where it is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,5-Dimethoxy-4-ethoxyamphetamine
2,5-Dimethoxy-4-ethoxyamphetamine (MEM) is a psychedelic drug of the phenethylamine and amphetamine chemical classes. It was first synthesized by Alexander Shulgin. In his book '' PiHKAL'', he lists the active dose range as 20–50 mg, and the duration as 10–14 hours. According to Shulgin, MEM produces color enhancement, visual phenomena, and pattern movement, among other effects. MEM possesses affinity (Ki) for the 5-HT2A (3,948 nM), 5-HT2B (64.5 nM), 5-HT7 (7,156 nM), and σ1 (5,077 nM) receptors. It behaves as a partial agonist at the 5-HT2A receptor. MEM is relatively selective for these sites and displays low/negligible (> 10,000 nM) affinity for a wide array of other targets. See also * 2,5-Dimethoxy-4-substituted amphetamine 4-Substituted-2,5-dimethoxyamphetamines (DO''x'') is a chemical class of substituted amphetamine derivatives featuring methoxy groups at the 2- and 5- positions of the phenyl ring, and a substituent such as alkyl or halogen at th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methylenedioxyamphetamine
3,4-Methylenedioxyamphetamine (also known as MDA and sass) is an empathogen-entactogen, psychostimulant, and psychedelic drug of the amphetamine family that is encountered mainly as a recreational drug. In terms of pharmacology, MDA acts most importantly as a serotonin–norepinephrine–dopamine releasing agent (SNDRA). In most countries, the drug is a controlled substance and its possession and sale are illegal. MDA is rarely sought after as a recreational drug compared to other drugs in the amphetamine family; however, it remains an important and widely used drug due to it being a primary metabolite, the product of hepatic N-dealkylation, of MDMA (ecstasy). In addition, it is common to find MDA as an adulterant of illicitly produced MDMA. Uses Medical MDA currently has no accepted medical use. Recreational MDA is bought, sold, and used as a recreational 'love drug', due to its enhancement of mood and empathy. A recreational dose of MDA is sometimes cited as bei ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-2A Adrenergic Receptor
The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the human gene encoding it. Receptor α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mice revealed that both the α2A and α2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the α2A subtype inhibited transmitter release at high stimulation frequencies, whereas the α2C subtype modulated neurotransmission at lower levels of nerve activity Gene This gene encodes α2A subtype and it contains no introns in either its coding or untranslated sequences. Role in central nervous system Although the pre-synaptic functions of α2A receptors are often a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanfacine
Guanfacine, sold under the brand name Tenex among others, is an oral medication used to treat attention deficit hyperactivity disorder (ADHD) and high blood pressure. Guanfacine is FDA-approved for monotherapy treatment of ADHD as well as being used for augmentation of other treatments, such as stimulants. Guanfacine is also used off-label to treat tic disorders, anxiety disorders and PTSD.Boland, Robert and Verduin, Marcia (2022) ''Kaplan & Sadock's Concise Textbook of Clinical Psychiatry''. 5th ed. pp. 1811–1812. Common side effects include sleepiness, constipation, and dry mouth. Other side effects may include low blood pressure and urinary problems. The FDA has categorized Guanfacine as "Category B" in pregnancy which means animal-reproduction studies have not demonstrated a fetal risk or an adverse effect during pregnancy or breastfeeding. It appears to work by activating the α2A receptors in the brain thereby decreasing sympathetic nervous system activity. Guanfac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
