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IHCH-7113
IHCH-7113 is a drug which acts as an agonist at the 5-HT2A receptor, 5-HT2A serotonin Receptor (biochemistry), receptor. It was derived by structural simplification of the 5-HT2A antagonist atypical antipsychotic drug lumateperone along with several related compounds such as IHCH-7079 and IHCH-7086, which were found to be nonhallucinogenic biased 5-HT2A agonists that were active in antidepressant assays but did not produce psychedelic-like responding in mice. IHCH-7113 however produced a head-twitch response comparable to that of 2,5-Dimethoxy-4-iodoamphetamine, DOI or LSD, which was blocked by the 5-HT2A antagonist MDL100907. yrrolo [1,2,3-de]quinoxalin-8-(7H ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AAZ-A-154
AAZ-A-154 is a novel isotryptamine derivative which acts as a 5-HT2A receptor, 5-HT2A receptor agonist discovered and synthesized by the lab of Professor David E. Olson at University of California, Davis, UCDavis. Animal studies suggest that it produces antidepressant effects without the psychedelic action typical of drugs from this class. In tests, AAZ-A-154 had antidepressant effects in mice without causing the head-twitch response linked to hallucinogenic effects. Due to the rapidly-induced and enduring neuroplasticity, AAZ-A-154 is a member of the class of compounds known as non-hallucinogenic psychoplastogens. This compound, as well as related compounds, are licensed by Delix Therapeutics and are being developed as potential medicines for Mental disorder, neuropsychiatric disorders. See also * α,N,N-Trimethyltryptamine * 5-MeO-DMT * 6-Fluoro-DET * AL-34662 * IHCH-7113 * (R)-69 * Neuroplasticity * Psychoplastogen * Delix Therapeutics * David E. Olson References Desi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WAY-163909
WAY-163,909 is a drug which acts as a potent and reasonably selective agonist for the serotonin 5-HT2C receptor. It has antipsychotic-like effects in animal models, and has been used to study the role of the 5-HT2C receptor subtype in the action of addictive drugs such as nicotine and methamphetamine. See also * IHCH-7113 * Lorcaserin * Ro60-0213 * Vabicaserin * 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-HT2C agonists Serotonin receptor agonists Heterocyclic compounds with 4 rings Benzodiazepines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SCHEMBL5334361
SCHEMBL5334361 is a drug which acts as an agonist at the 5-HT2 family of serotonin receptors, and was developed for the treatment of glaucoma. It is a benzazepine derivative structurally related to the anorectic drug lorcaserin. It is selective for 5-HT2A, with an EC50 of 0.4nM at 5-HT2A vs 3.9nM at 5-HT2C and a much lower affinity of 417nM at 5-HT2B. See also * 3C-BZ * AAZ-A-154 * AL-34662 * GSK-189254 * IHCH-7113 * O-4310 O-4310 (1-isopropyl-6-fluoro-psilocin) is a tryptamine derivative developed by Organix Inc which acts as a serotonin receptor agonist. It is claimed to have an EC50 of 5nM at 5-HT2A with 89% efficacy vs 5-HT, and 100x selectivity over 5-HT2C, ... References Serotonin receptor agonists Benzazepines O-methylated phenols {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RH-34
RH-34 is a compound which acts as a potent and selective partial agonist for the 5-HT2A serotonin receptor subtype. It was derived by structural modification of the selective 5-HT2A antagonist ketanserin, with the 4-(p-fluorobenzoyl)piperidine moiety replaced by the ''N''-(2-methoxybenzyl) pharmacophore found in such potent 5-HT2A agonists as NBOMe-2C-B and NBOMe-2C-I. This alteration was found to retain 5-HT2A affinity and selectivity, but reversed activity from an antagonist to a moderate efficacy partial agonist. Legal status RH-34 is a controlled substance in Hungary and Brazil. See also * 5-MeO-NBpBrT * IHCH-7113 * Ketanserin Ketanserin ( INN, USAN, BAN) (brand name Sufrexal; former developmental code name R41468) is a drug used clinically as an antihypertensive agent and in scientific research to study the serotonin system; specifically, the 5-HT2 receptor family. I ... * Efavirenz References {{Serotonergics Amines Quinazolines Serotonin receptor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherwis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
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] |
NDTDI
NDTDI is a tricyclic tryptamine derivative which is thought to act as a serotonin receptor agonist, though its pharmacology has not been studied in detail. It is a structurally simplified analogue of LSD and is reported to retain similar effects, though with many times lower potency. It has been sold as a designer drug since 2016 and was first identified by a forensic laboratory in Slovenia in 2017. Legality NDTDI was made illegal in Latvia in March 2017. See also * 4,5-DHP-DMT * Bay R 1531 * RU-28306 RU-28306 is a tricyclic tryptamine derivative which acts as a serotonin receptor agonist, with selectivity for 5-HT1 and 5-HT2 subtypes. It can be regarded either as a conformationally constrained derivative of DMT, or a structurally simplifi ... * RU-24,969 References {{Tryptamines Serotonin receptor agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mefloquine
Mefloquine, sold under the brand name Lariam among others, is a medication used to prevent or treat malaria. When used for prevention it is typically started before potential exposure and continued for several weeks after potential exposure. It can be used to treat mild or moderate malaria but is not recommended for severe malaria. It is taken by mouth. Common side effects include vomiting, diarrhea, headaches, sleep disorders, and a rash. Serious side effects include potentially long-term mental health problems such as depression, hallucinations, and anxiety and neurological side effects such as poor balance, seizures, and ringing in the ears. It is therefore not recommended in people with a history of mental health problems or epilepsy. It appears to be safe during pregnancy and breastfeeding. Mefloquine was developed by the United States Army in the 1970s and came into use in the mid-1980s. It is on the World Health Organization's List of Essential Medicines. It is availa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lisuride
Lisuride, sold under the brand name Dopergin among others, is a monoaminergic medication of the ergoline class which is used in the treatment of Parkinson's disease, migraine, and high prolactin levels. It is taken by mouth. Side effects of lisuride include nausea and decreased blood pressure, among others. Lisuride acts as a mixed agonist and antagonist of dopamine, serotonin, and adrenergic receptors. Activation of specific dopamine receptors is thought to be responsible for its effectiveness in the treatment of Parkinson's disease and ability to suppress prolactin levels, while interactions with serotonin receptors are thought to be principally involved in its effectiveness for migraine. Medical uses Lisuride is used to lower prolactin and, in low doses, to prevent migraine attacks. The use of lisuride as initial antiparkinsonian medication for Parkinson's disease has been advocated, delaying the need for levodopa until lisuride becomes insufficient for controlling the park ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Efavirenz
Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention after a needlestick injury or other potential exposure. It is sold both by itself and in combination as efavirenz/emtricitabine/tenofovir. It is taken by mouth. Common side effects include rash, nausea, headache, feeling tired, and trouble sleeping. Some of the rashes may be serious such as Stevens–Johnson syndrome. Other serious side effects include depression, thoughts of suicide, liver problems, and seizures. It is not safe for use during pregnancy. It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and works by blocking the function of reverse transcriptase. Efavirenz was approved for medical use in the United States in 1998, and in the European Union in 1999. It is on the World Health Organization's List of Essential Medicines. A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MDL100907
Volinanserin (INN) (developmental code name MDL-100,907) is a highly selective 5-HT2A receptor antagonist that is frequently used in scientific research to investigate the function of the 5-HT2A receptor. It was also tested in clinical trials as a potential antipsychotic, antidepressant, and treatment for insomnia but was never marketed. See also * Glemanserin * Pruvanserin * Roluperidone * Lenperone * Lidanserin * Ketanserin * Ritanserin * Eplivanserin Eplivanserin (SR-46,349; planned trade name Ciltyri) was an experimental drug for the treatment of insomnia which was being developed by Sanofi Aventis. Sanofi Aventis announced in December 2009 that it was withdrawing its application for approv ... * Pimavanserin References 5-HT2A antagonists Fluoroarenes Piperidines Secondary alcohols Phenol ethers Abandoned drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
