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Ro 60-0175
Ro60-0175, also known as (''S'')-5,6-difluoroindolmethylethylamine, is a serotonin receptor agonist of the isotryptamine group developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective agonist of both the serotonin 5-HT2B and 5-HT2C receptor subtypes, with good selectivity over the closely related serotonin 5-HT2A subtype, and little or no affinity at other receptors. However, Ro60-0175 also activates the serotonin 5-HT2A receptor less potently than the serotonin 5-HT2B and 5-HT2C receptors. In combination with the selective serotonin 5-HT2C receptor antagonist SB-242084, Ro60-0175 robustly induces the head-twitch response, a behavioral proxy of psychedelic effects, in rodents. This effect is abolished by addition of the selective serotonin 5-HT2A receptor antagonist ketanserin or volinanserin. The preceding findings suggest that Ro60-0175 may be a serotonergic psychedelic and may have hallucinogenic effects in humans ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonist
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors. Non-selective agonists Serotonergic psychedelics such as tryptamines (e.g., psilocybin, psilocin, , 5-MeO-DMT, bufotenin), lysergamides (e.g., , ergine ()), phenethylamines (e.g., mescaline, 2C-B, 25I-NBOMe), and amphetamines (e.g., , ) are non-selective agonists of serotonin receptors. Their hallucinogenic effects are specifically mediated by activation of the 5-HT2A receptor. Drugs that increase extracellular serotonin levels such as serotonin reuptake inhibitors (e.g., fluoxetine, venlafaxine), serotonin releasing agents (e.g., fenfluramine, ), and monoamine oxidase inhibitors (e.g., phenelzine, moclobemide) are indirect non-selective serotonin receptor agonists. They are used variously as antidepressant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketanserin
Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospasm, vasospastic disorders. It is also used in scientific research as an antiserotonergic medication, agent in the study of the serotonin system; specifically, the 5-HT2 receptor, 5-HT2 receptor family. The drug is taken oral administration, by mouth. Side effects of ketanserin include dizziness, tiredness, edema, dry mouth, weight gain, and drug-induced QT prolongation, QT interval prolongation. Ketanserin acts as a binding selectivity, selective receptor antagonist, antagonist of the serotonin 5-HT2A receptor, 5-HT2A, α1-adrenergic receptor, α1-adrenergic, and histamine H1 receptor, H1 receptors. It also shows lower affinity (pharmacology), affinity for various other biological target, targets. Ketanserin was discovered at Janssen Pharmaceutica in 1980. It was the first serotonin 5-HT2A receptor antagonist to be discovered that showed selectiv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs Developed By Hoffmann-La Roche
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or 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 treat, cure, prevent, or 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 for a limited duration, or on a regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that have simila ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2C Agonists
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and v ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 * ''O''-Methyl-AL-34662 * Ro60-0175 * VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT ... References Amines Serotonin receptor agonists Indazoles Benzofurans Heterocyclic compounds with 3 rings Nitrogen heterocycles Oxygen heterocycles {{nervous-system-drug-stub ... [...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 receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT2A receptor, 5-HT2A. It has potent anorectic effects in animal studies. See also * α-Methylisotryptamine * AL-34662 * AL-38022A * Ro60-0175 * VU6067416 * YM-348 References 5-HT2B agonists Serotonin receptor agonists Indolines Bromoarenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro60-0213
Ro60-0213 (Org 35032) is a drug developed by Hoffmann–La Roche, which acts as a potent and selective agonist for the 5-HT2C serotonin receptor, with more than 100x selectivity over other closely related serotonin receptor subtypes, and little or no affinity at other receptors. It was developed as a potential antidepressant, but was discontinued from clinical development at an early stage due to toxicity concerns. However the high selectivity of Ro60-0213 for 5-HT2C makes it of continued interest for research into serotonin receptors. See also * 5-MeO-AMT * AL-34662 * AL-38022A * Ro60-0175 * VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT ... * YM-348 References Serotonin receptor agonists Drugs developed by Hoffmann-La Roche Indenes Methoxy compounds { ... [...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 such as in the treatment of glaucoma. 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 four times 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 * ''O''-Methyl-AL-34662 * Ro60-0175 * VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT ... * YM-348 References Amines Indazoles Dihydropyrans Psychedelic drugs Serotonin receptor agonists Heterocyclic compounds with 3 rings {{A ... [...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 serotonin 5-HT2 receptor agonist, including of the 5-HT2A, 5-HT2B, and 5-HT2C receptors (affinity () = 14.5, 8.1, and 3.0nM, respectively). The serotonin 5-HT2A receptor is the same target as that of psychedelic drugs like psilocin. Unlike these drugs however, 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 receptor agonists, namely reduction in intra-ocular pressure and hence relief from the symptoms of glaucoma, but without causing the psychedelic effects that make centrally active serotonin 5-HT2A receptor 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
