|
Acetryptine
Acetryptine (International Nonproprietary Name, INN; developmental code W-2965-A; also known as 5-acetyltryptamine or 5-AT) is a drug described as an antihypertensive agent which was never marketed. Structurally, acetryptine is a substituted tryptamine, and is closely related to other substituted tryptamines like serotonin (5-hydroxytryptamine). It was developed in the early 1960s. The receptor binding, binding of acetryptine to serotonin receptors does not seem to have been well-investigated, although it was assessed at the 5-HT1A receptor, 5-HT1A and 5-HT1D receptor, 5-HT1D receptors and found to bind to them with high affinity (pharmacology), affinity. The drug may also act as a monoamine oxidase inhibitor (MAOI); specifically, as an enzyme inhibitor, inhibitor of MAO-A. See also * 5-Benzyloxytryptamine * 5-Carboxamidotryptamine * 5-Ethoxy-DMT * 5-Methoxytryptamine * 5-Methyltryptamine * 5-(Nonyloxy)tryptamine * Azepindole * Indorenate * Metralindole * Pargyline * Pirlindole * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tryptamines
Substituted tryptamines, or simply tryptamines, also known as serotonin analogues (i.e., 5-hydroxytryptamine analogues), are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino group, amino (NH2) group via an ethyl (−CH2–CH2−) side chain, sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and dimethyltryptamine, DMT. In South America, dimethyltryptamine is obtained f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indorenate
Indorenate (TR-3369), is a tryptamine derivative which acts as an agonist at the 5-HT1A, 5-HT1B and 5-HT2C serotonin receptors. It has anxiolytic, antihypertensive and anorectic effects, predominantly through action at 5-HT1A, but with some contribution from the 5-HT1B and 5-HT2C subtypes, and possibly some other non-serotonergic targets also. See also * 5-Methoxytryptamine * Acetryptine Acetryptine (International Nonproprietary Name, INN; developmental code W-2965-A; also known as 5-acetyltryptamine or 5-AT) is a drug described as an antihypertensive agent which was never marketed. Structurally, acetryptine is a substituted tryp ... References Serotonin receptor agonists 5-Methoxytryptamines Methyl esters Carboxylate esters {{anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Carboxamidotryptamine
5-Carboxamidotryptamine (5-CT) is a tryptamine derivative closely related to the neurotransmitter serotonin. 5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as an agonist of the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has negligible affinity for the 5-HT1E and 5-HT1F receptors. 5-CT binds most strongly to the 5-HT1A receptor and it was once thought to be selective for this site. Recently, a close derivative of 5-CT, AH-494 has been shown to function as an agonist of 5-HT7, although being more selective over 5-HT1A. Structural study indicated residue Ser5x43 might play critical roles in the selectivity of 5-CT across the serotonin receptor family. See also * 2-Methyl-5-hydroxytryptamine * 5-Benzyloxytryptamine * 5-Methoxytryptamine * 5-Methyltryptamine * α-Methyl-5-hydroxytryptamine * Frovatriptan * AH-494 * Acetryptine * Sumatriptan Sumatriptan, sold under th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
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 vas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Methyltryptamine
5-Methyltryptamine (5-MeT, 5-Me-T) is a non-selective serotonin receptor agonist and serotonin releasing agent of the tryptamine family that has been used in scientific research. It is related to other 5-substituted tryptamines such as serotonin (5-hydroxytryptamine; 5-HT) and 5-methoxytryptamine (5-MeO-T). The compound is also a positional isomer of ''N''-methyltryptamine (NMT). Pharmacology 5-MeT is known to act as a potent serotonin 5-HT2A receptor full agonist, with an of 6.00nM and an of 100%. In addition, it is known to be a ligand of the serotonin 5-HT1A and 5-HT2B receptors and an agonist of the serotonin 5-HT1D and 5-HT2C receptors. Similarly to tryptamine and 5-MeO-T, but in contrast to serotonin, 5-MeT shows very low potency as an agonist of the serotonin 5-HT3 receptor ( = 60,000nM). In addition to acting as an agonist of various serotonin receptors, 5-MeT is a monoamine releasing agent (MRA), with high selectivity for induction of serotonin release over i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Agonists
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 an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihypertensive Agents
Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke, heart failure, kidney failure and myocardial infarction. Evidence suggests that a reduction of blood pressure by 5 mmHg can decrease the risk of stroke by 34% and of ischaemic heart disease by 21%. It can reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used medications are thiazide diuretics, calcium channel blockers, angiotensin-converting enzyme inhibitors (ACE inhibitors), angiotensin II receptor blockers or antagonists (ARBs), and beta blockers. Which type of medication to use initially for hypertension has been the subject of several large studies and resulting national guidelines. The fundamental g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrindole
Tetrindole was a drug candidate that functions by reversibly inhibiting monoamine oxidase A; it was first synthesized in Moscow in the early 1990s. Tetrindole is similar in its chemical structure to pirlindole (Pyrazidol), and metralindole. See also * List of Russian drugs This page is a list of Russian drugs, or drugs that were developed in Russia, the former Soviet Union, and/or post-Soviet countries. Many Russian drugs are indicated for enhancing physical, mental, and/or cognitive performance, including drugs ... References Carbazoles Reversible inhibitors of MAO-A Abandoned drugs Monoamine oxidase inhibitors Russian drugs Cyclohexyl compounds Substances discovered in the 1990s {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sumatriptan
Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches. It is taken Oral administration, orally, Nasal administration, intranasally, or by Subcutaneous injection, subcutaneous Injection under the skin, injection. Therapeutic effects generally occur within three hours. Its primary effect as a serotonin 5-HT1B, 5-HT1B/5-HT1D receptor, 5-HT1D receptor agonist can create common side effects such as chest pressure, fatigue, vomiting, tingling, and vertigo. Serious side effects may include serotonin syndrome, heart attack, stroke, and seizures. With excessive use, medication overuse headaches may occur. It is unclear if use during pregnancy or breastfeeding is safe. The mechanism of action is not entirely clear. It is in the triptan class of medications. Sumatriptan was patented in 1982 and approved for medical use in 1991. It is on the WHO Model List of Essential Medicines, World Health Organization's L ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pirlindole
Pirlindole, sold under the brand names Lifril and Pyrazidol, is mainly a reversible inhibitor of monoamine oxidase A (RIMA) and secondly a serotonin–norepinephrine reuptake inhibitor (SNRI) which was developed and is used in Russia as an antidepressant. It is structurally and pharmacologically related to metralindole. Synthesis The Fischer indole synthesis between ''p''-Tolylhydrazine Hydrochloride 37-60-5(1) and 1,2-Cyclohexanedione 65-87-7(2) gives 6-methyl-2,3,4,9-tetrahydrocarbazol-1-one 449-48-7(3). Imine formation with ethanolamine 41-43-5(4) giveCID:2838578(5). Halogenation with phosphorus oxychloride gives (6). Intramolcular alkylation with the indole nitrogen resulted in Dehydropirlindole 5804-32-9(7). Reduction of the imine with sodium borohydride completes the synthesis of pirlindole (8). See also * Metralindole * Tetrindole * List of Russian drugs This page is a list of Russian drugs, or drugs that were developed in Russia, the former Soviet Union, and/o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pargyline
Pargyline, sold under the brand name Eutonyl among others, is a monoamine oxidase inhibitor (MAOI) medication which has been used to treat hypertension (high blood pressure) but is no longer marketed. It has also been studied as an antidepressant, but was never licensed for use in the treatment of depression. The drug is taken by mouth. Side effects of pargyline include orthostatic hypotension among others. It has the potential for serious food and drug interactions with sympathomimetic agents like tyramine that can result in hypertensive crisis. Pargyline acts as a non-selective and irreversible inhibitor of the monoamine oxidases MAO-A and MAO-B. The exact mechanism of the hypotensive effects of pargyline and other MAOIs is unclear. Structurally, pargyline is a benzylamine derivative and is related to selegiline and clorgyline. Pargyline was first described in 1960 and was introduced for medical use in 1963. It was available in the United States and the United Kingdom. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
