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Acetryptine
Acetryptine (INN) (developmental code name W-2965-A), also known as 5-acetyltryptamine (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 binding of acetryptine to serotonin receptors does not seem to have been well-investigated, although it was assessed at the 5-HT1A and 5-HT1D receptors and found to bind to them with high affinity. The drug may also act as a monoamine oxidase inhibitor (MAOI); specifically, as an inhibitor of MAO-A. See also * 5-Benzyloxytryptamine * 5-Carboxamidotryptamine * 5-Ethoxy-DMT * 5-Methoxytryptamine * 5-(Nonyloxy)tryptamine * Azepindole * Indorenate * Metralindole * Pargyline * Pirlindole * Sumatriptan Sumatriptan, sold commonly under brand names Imitrex and Treximet among others, is a medication used to treat m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Tryptamine
Substituted tryptamines, or serotonin 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 (NH2) group via an ethyl (−CH2–CH2−) 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 DMT. In South America, dimethyltryptamine is obtained from numerous plant sources, like chacruna, and it is often used in ayahuasca brews. Many synthetic tryptamines ... [...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 at 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 * α-Methyl-5-hydroxytryptamine * Frovatriptan Frovatriptan, sold under the brand name Frova, is a triptan drug developed by Vernalis for the treatmen ... [...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 (INN) (developmental code name W-2965-A), also known as 5-acetyltryptamine (5-AT), is a drug described as an antihypertensive agent which was never marketed. Structurally, acetryptine is a substituted tryptamine, and is closely relat ... References Serotonin receptor agonists Mexamines Methyl esters Carboxylate esters {{nervous-system-drug-stub ... [...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 and myocardial infarction. Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34% and of ischaemic heart disease by 21%, and 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, ACE inhibitors, angiotensin II receptor 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 goal of treatment should be the prevention of the important endpoints of hypertension, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrindole
Tetrindole was a drug candidate that functions by reversibly inhibiting monoamine oxidase A Monoamine oxidase A, also known as MAO-A, is an enzyme that in humans is encoded by the ''MAOA'' gene. This gene is one of two neighboring gene family members that encode mitochondrial enzymes which catalyze the oxidative deamination of amines, ...; it was first synthesized in Moscow in the early 1990s. Tetrindole is similar in its chemical structure to pirlindole (Pyrazidol), and metralindole. 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 commonly under brand names Imitrex and Treximet among others, is a medication used to treat migraine headaches and cluster headaches. It is taken orally, intranasally, or by subcutaneous injection. Therapeutic effects generally occur within three hours. Its primary effect as a serotonin 5-HT1B/1D receptor agonist can create common side effects such as chest pressure, fatigue, vomiting, tingling, and vertigo. Serious side effects may include serotonin syndrome, heart attacks, strokes, and seizures. With excessive medication overuse headaches may occur. It is unclear if use during pregnancy or breastfeeding is safe. The mechanism of action 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 World Health Organization's List of Essential Medicines. It is available as a generic medication. In 2020, it was the 111th most commonly prescribed medication in the United ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pirlindole
Pirlindole (Lifril, Pyrazidol) is mainly a reversible inhibitor of monoamine oxidase A (RIMA) and secondly a 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 ' (8). See also * Metralindole * Tetrindole Tetrindole was a drug candidate that functions by reversibly inhibiting monoamine oxidase A Monoamine oxidase A, also known as MAO-A, is an enzyme that in humans is encoded by the ''MAOA'' gene. This gene is one of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pargyline
Pargyline (brand name Eutonyl) is an irreversible selective monoamine oxidase (MAO)-B inhibitor drug ( IC50 for MAO-A is 0.01152 μmol/L and for MAO-B is 0.00820 μmol/L) It was brought to market in the US and the UK by Abbott in 1963 as an antihypertensive drug branded "Eutonyl". It was one of several MAO inhibitors introduced in the 1960s including nialamide, isocarboxazid, phenelzine, and tranylcypromine. By 2007 the drug was discontinued and as of 2014 there were no generic versions available in the US. In addition to its actions as an MAOI, pargyline has been found to bind with high affinity to the I2 imidazoline receptor (an allosteric site on the MAO enzyme). See also * Clorgyline * Rasagiline Rasagiline (Azilect, Azipron) is an irreversible inhibitor of monoamine oxidase-B used as a monotherapy to treat symptoms in early Parkinson's disease or as an adjunct therapy in more advanced cases. The racemic form of the drug was invented b ... * Selegiline Refer ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metralindole
Metralindole (Inkazan) is a reversible inhibitor of monoamine oxidase A (RIMA) which was investigated in Russia as a potential antidepressant. It is structurally A structure is an arrangement and organization of interrelated elements in a material object or system, or the object or system so organized. Material structures include man-made objects such as buildings and machines and natural objects such as ... and pharmacologically related to pirlindole. See also * Pirlindole * Tetrindole References beta-Carbolines Tryptamines Reversible inhibitors of MAO-A Antidepressants Monoamine oxidase inhibitors Russian drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azepindole
Azepindole (McN-2453) is a tricyclic compound with antidepressant and antihypertensive effects that was developed in the late 1960s but was never marketed. See also * Tricyclic antidepressant Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants, which is important for the management of depression. They are second-line drugs next to SSRIs. TCAs were discovered in the early 1950s and wer ... References Tricyclic antidepressants Diazepines Indoles Abandoned drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-(Nonyloxy)tryptamine
5-(Nonyloxy)tryptamine is a tryptamine derivative which acts as a selective agonist at the 5-HT1B receptor. Increasing the O-alkoxy chain length in this series gives generally increasing potency and selectivity for 5-HT1B, with highest activity found for the nonyloxy derivative, having a 5-HT1B binding affinity of 1.0 nM, and around 300-fold selectivity over the related 5-HT1A receptor. See also * 5-Benzyloxytryptamine * 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 a ... * 5-Ethoxy-DMT * Sumatriptan References Serotonin receptor agonists Tryptamines Indole ethers at the benzene ring {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
