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ORG-37,684
ORG-37684 is a drug developed by Organon, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Partn ... at 5-HT2C and lowest at 5-HT2B subtypes. It has anorectic effects in animal studies and has been researched as a potential weight loss drug for use in humans. See also * ORG-12962 * Quipazine References Serotonin receptor agonists Indanes Phenol ethers Pyrrolidines {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2C Receptor
The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gq/G11 and mediates excitatory neurotransmission. ''HTR2C'' denotes the human gene encoding for the receptor, that in humans is located at the X chromosome. As males have one copy of the gene and in females one of the two copies of the gene is repressed, polymorphisms at this receptor can affect the two sexes to differing extent. Structure At the cell surface the receptor exists as a homodimer. The crystal structure is known since 2018. Distribution 5-HT2C receptors are located mainly in the choroid plexus, and in rats is also found in many other brain regions in high concentrations, including parts of the hippocampus, anterior olfactory nucleus, substantia nigra, several brainstem nuclei, amygdala, subthalamic nucleus and lateral habenula. 5-HT2C receptors are also found on epithel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2B Receptor
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, medial ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonists
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is rel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quipazine
Quipazine is a serotonergic drug of the piperazine group which is used in scientific research. It was originally intended as an antidepressant but never developed for medical use. Pharmacology Pharmacodynamics Quipazine is a serotonin reuptake inhibitor, and also a moderately selective serotonin receptor agonist, binding to a range of different serotonin receptors, but particularly to the 5-HT2A and 5-HT3 subtypes. Quipazine produces a head-twitch response and other psychedelic-consistent effects in animal studies including in mice, rats, and monkeys. However, it failed to produce psychedelic effects in humans at a dose of 25 mg, which was the highest dose tested due to 5-HT3 mediated side effects of nausea and gastrointestinal discomfort. However Alexander Shulgin claimed that a fully effective psychedelic dose could be reached by blocking 5-HT3 receptors using a 5-HT3 antagonist. Chemistry Quipazine is synthesized by reacting 2-chloroquinoline with piperazine. S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ORG-12962
ORG-12962 is a pyridinylpiperazine drug developed by Organon, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity at 5-HT2C and lowest at 5-HT2B subtypes. It was developed as a potential anti-anxiety drug, but was discontinued from human trials after tests in a public speaking challenge showed that its anti-anxiety effects were accompanied by side effects such as dizziness and a "spacey" feeling, which were attributed to poor selectivity ''in vivo'' over the hallucinogenic 5-HT2A receptor. Synthesis Note that patent serves to deliver 1- -chloro-5-(trifluoromethyl)pyridin-2-yliperazine 32834-59-4 although patent is correct oneCID:9796408 Hence, ORG-12962, would need 2,6-Dichloro-3-(trifluoromethyl)pyridine 5304-75-1 2,3-dichloro-5-trifluoromethylpyridine 9045-84-7 See also * 2C-B-PP * 2,3-Dichlorophenylpiperazine * 3-Chloro-4-fluorophenylpiperazine * CPD-1 * ORG-37684 * Quipazine Quipazine is a serotonergic drug of the pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Weight Loss
Weight loss, in the context of medicine, health, or physical fitness, refers to a reduction of the total body mass, by a mean loss of fluid, body fat (adipose tissue), or lean mass (namely bone mineral deposits, muscle, tendon, and other connective tissue). Weight loss can either occur unintentionally because of malnourishment or an underlying disease, or from a conscious effort to improve an actual or perceived overweight or obese state. "Unexplained" weight loss that is not caused by reduction in calorific intake or exercise is called cachexia and may be a symptom of a serious medical condition. Intentional Intentional weight loss is the loss of total body mass as a result of efforts to improve physical fitness, fitness and health, or to change Human physical appearance, appearance through slimming. Weight loss is the main Management of obesity, treatment for obesity, and there is substantial evidence this can prevent progression from prediabetes to Diabetes mellitus, ty ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anorectic
An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek ''ἀν-'' (an-) = "without" and ''ὄρεξις'' (órexis) = "appetite"), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term basis clinically to treat obesity, some appetite suppressants are also available over-the-counter. Most common natural appetite suppressants are based on ''Hoodia'', a genus of 13 species in the flowering plant family Apocynaceae, under the subfamily Asclepiadoideae. Several appetite suppressants are based on a mix of natural ingredients, mostly using green tea as its basis, in combination with other plant extracts such as fucoxanthin, found naturally in seaweed. Drugs of this class are frequently stimulants of the phenethylamine family, related to amphetamine. The German and Fi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Organon International
Organon & Co. is an American pharmaceutical company headquartered in Jersey City, New Jersey. Organon specializes in the following core therapeutic fields: reproductive medicine, contraception, psychiatry, hormone replacement therapy (HRT), and anesthesia. Organon sells to international markets. History Organon was founded by Dr. Saal van Zwanenberg in Oss, the Netherlands, in 1923 as a separate part of the meat factory Zwanenberg's fabrieken. Its first product was insulin in 1923. In the thirties it manufactured estrogens. In 1948, Organon acquired the Newhouse research site in Scotland, United Kingdom. The production of cortisone was initiated in 1953. In 1962, it bought the stock of the Nederlandsche Cocaïnefabriek. The company name was changed to Koninklijke Zwanenberg-Organon (KZO), and it merged with the fibre producer AKU in 1969 to become AKZO, later Akzo Nobel. Organon was the human health care business unit of Akzo Nobel. In 2004, Organon acquired active-pharmace ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition of liga ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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