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YM-348
YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor. It has thermogenic and anorectic effects in animal studies, making it potentially useful for the treatment of obesity. See also * AL-34662 * AL-38022A * Ro60-0175 * VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT2A. It has potent anorectic effects in animal studies. ... References Amines Serotonin receptor agonists Indazoles Benzofurans Heterocyclic compounds with 3 rings {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AL-34662
AL-34662 is an indazole derivative drug that is being developed for the treatment of glaucoma. It acts as a selective 5-HT2A receptor agonist, the same target as that of psychedelic drugs like psilocin, but unlike these drugs, AL-34662 was designed specifically as a peripherally selective drug, which does not cross the blood–brain barrier. This means that AL-34662 can exploit a useful side effect of the hallucinogenic 5-HT2A agonists, namely reduction in intra-ocular pressure and hence relief from the symptoms of glaucoma, but without causing the hallucinogenic effects that make centrally active 5-HT2A agonists unsuitable for clinical use. In animal studies, AL-34662 has been shown to be potent and effective in the treatment of symptoms of glaucoma, with minimal side effects. Peripherally acting 5-HT2A agonists have been a rich field of research in recent years, with potential glaucoma treatments being the main proposed application for 5-HT2A agonists at present, as centrally ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
VER-3323
VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT2A. It has potent anorectic effects in animal studies. See also * AL-34662 * AL-38022A * Ro60-0175 * YM-348 YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor. ... References 5-HT2B agonists Serotonin receptor agonists Indolines Bromoarenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro60-0175
Ro60-0175 is a drug developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with good selectivity over the closely related 5-HT2A subtype, and little or no affinity at other receptors. See also * AL-34662 * AL-38022A * Ro60-0213 * VER-3323 * YM-348 YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor. ... References 5-HT2B agonists Serotonin receptor agonists Indoles Chloroarenes Fluoroarenes Hoffmann-La Roche brands {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AL-38022A
AL-38022A is an indazole derivative drug which is one of a range of similar drugs developed for scientific research and with some possible clinical applications. It acts as a potent and selective agonist for the 5-HT2 family of serotonin receptors, with highest binding affinity for the 5-HT2C subtype and around 4x less affinity for 5-HT2A and 5-HT2B. In drug discrimination tests on animals, it fully substituted for both DOM and 5-MeO-DMT. See also * AL-34662 * AL-37350A * Ro60-0175 * VER-3323 * YM-348 YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor. ... References Amines Indazoles Dihydropyrans Serotonin receptor agonists Heterocyclic compounds with 3 rings {{Amine-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] |
Indazole
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole. Indazole is an amphoteric molecule which can be protonated to an indazolium cation or deprotonated to an indazolate anion. The corresponding ''pKa'' values are 1.04 for the equilibrium between indazolium cation and indazole and 13.86 for the equilibrium between indazole and indazolate anion. Indazole derivatives display a broad variety of biological activities. Indazoles are rare in nature. The alkaloids nigellicine, nigeglanine, and nigellidine are indazoles. Nigellicine was isolated from the widely distributed plant ''Nigella sativa'' L. (black cumin). Nigeglanine was isolated from extracts of ''Nigella glandulifera''. The Davis–Beirut reaction can generate 2''H''-indazoles. Indazole, C7H6N2, was obtained by E. Fischer (''Ann.'' 1883, 221, p. 280) by heating ortho-hydrazine cinnamic acid, : Some derivatives ; indazole-3- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indazoles
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole. Indazole is an Amphoterism, amphoteric molecule which can be protonated to an indazolium cation or deprotonated to an indazolate anion. The corresponding ''pKa'' values are 1.04 for the equilibrium between indazolium cation and indazole and 13.86 for the equilibrium between indazole and indazolate anion. Indazole derivatives display a broad variety of biological activities. Indazoles are rare in nature. The alkaloids nigellicine, nigeglanine, and nigellidine are indazoles. Nigellicine was isolated from the widely distributed plant ''Nigella sativa'' L. (black cumin). Nigeglanine was isolated from extracts of ''Nigella glandulifera''. The Davis–Beirut reaction can generate 2''H''-indazoles. Indazole, C7H6N2, was obtained by E. Fischer (''Ann.'' 1883, 221, p. 280) by heating ortho-hydrazine cinnamic acid, : Some derivatives ; i ... [...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] |
Amines
In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines). Important amines include amino acids, biogenic amines, trimethylamine, and aniline; Inorganic derivatives of ammonia are also called amines, such as monochloramine (). The substituent is called an amino group. Compounds with a nitrogen atom attached to a carbonyl group, thus having the structure , are called amides and have different chemical properties from amines. Classification of amines Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Obesity
Obesity is a medical condition, sometimes considered a disease, in which excess body fat has accumulated to such an extent that it may negatively affect health. People are classified as obese when their body mass index (BMI)—a person's weight divided by the square of the person's height—is over ; the range is defined as overweight. Some East Asian countries use lower values to calculate obesity. Obesity is a major cause of disability and is correlated with various diseases and conditions, particularly cardiovascular diseases, type 2 diabetes, obstructive sleep apnea, certain types of cancer, and osteoarthritis. Obesity has individual, socioeconomic, and environmental causes. Some known causes are diet, physical activity, automation, urbanization, genetic susceptibility, medications, mental disorders, economic policies, endocrine disorders, and exposure to endocrine-disrupting chemicals. While a majority of obese individuals at any given time are attempting to ... [...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] |
Thermogenic
Thermogenic means tending to produce heat, and the term is commonly applied to drugs which increase heat through metabolic stimulation, or to microorganisms which create heat within organic waste. Approximately all enzymatic reaction in the human body is thermogenic, which gives rise to the basal metabolic rate.Yu‑Hua Tseng, Aaron M. Cypess and C. Ronald Kahn. Cellular bioenergetics as a target for obesity therapy. Reviews. Vol. 9. 2010: 465-81. In bodybuilding, athletes wishing to reduce body fat percentage use thermogenics in order to attempt to increase their basal metabolic rate, thereby increasing overall energy expenditure. Caffeine and ephedrine are commonly used for this purpose in the ECA stack. 2,4-Dinitrophenol (DNP) is a very strong thermogenic drug used for fat loss which produces a dose-dependent increase in body temperature, to the point where it can induce death by hyperthermia. It works as a mitochondrial oxidative phosphorylation uncoupler, disrupting the mitoc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
