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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] |
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, while being apparently inactive at the 5-HT2B antitarget. See also * 1-Methylpsilocin * 5-Fluoro-DMT * Psilocin * SCHEMBL5334361 * 7F-5-MeO-MET 5-MeO-7-F-MET (5-MeO-7F-MET, 5-Methoxy-7-fluoro-''N''-methyl-''N''-ethyltryptamine) is a tryptamine derivative which acts as a serotonin receptor agonist selective for the 5-HT2 subtypes, with a pEC50 of 8.71 at 5-HT2A, vs 8.25 at 5-HT2B and 7 ... References Tryptamines Fluoroarenes Isopropyl compounds Dimethylamino compounds Phenols {{Pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
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] |
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 |
3C-BZ
3C-BZ (4-benzyloxy-3,5-dimethoxyamphetamine) is a lesser-known psychedelic drug and a substituted amphetamine. 3C-BZ was first synthesized by Alexander Shulgin. In his book '' PiHKAL'', the dosage range is listed as 25–200 mg and the duration as 18–24 hours. According to anecdotal reports from the substance's entry in PiHKAL, 3C-BZ's effects can vary significantly, ranging from intensified emotions and strange dreams, to effects similar to those of LSD or TMA. Very little data exists about the pharmacological properties, metabolism, and toxicity of 3C-BZ. Synthesis 3C-BZ was originally synthesized by Alexander Shulgin starting from 5-methoxyeugenol (4-allyl-2,6-dimethoxyphenol) through a reaction with benzyl chloride to form the benzyloxy derivative of 5-methoxyeugenol. The obtained benzyl derivative was reacted with tetranitromethane to form 1- -(Benzyloxy)-3,5-dimethoxyphenyl2-nitro-1-propene, from which 3C-BZ is obtained by reduction of the nitropropene with lithiu ... [...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] |
GSK-189254
GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor ( Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia Dementia is a disorder which manifests as a set of related symptoms, which usually surfaces when the brain is damaged by injury or disease. The symptoms involve progressive impairments in memory, thinking, and behavior, which negatively affe ..., as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs. Referen ... [...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] |
5-HT2B Receptor
5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the ''HTR2B'' gene. 5-HT2B is a member of the 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Tissue distribution and function First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of hallucinogenic substituted amphetamines. The 5-HT2B receptor is expressed in several areas of the CNS, including the dorsal hypothalamus, frontal cortex, medial ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2 Receptor
The 5-HT2 receptors are a subfamily of 5-HT receptors that bind the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). The 5-HT2 subfamily consists of three G protein-coupled receptors (GPCRs) which are coupled to Gq/G11 and mediate excitatory neurotransmission Neurotransmission (Latin: ''transmissio'' "passage, crossing" from ''transmittere'' "send, let through") is the process by which signaling molecules called neurotransmitters are released by the axon terminal of a neuron (the presynaptic neuron), ..., including 5-HT2A, 5-HT2B, and 5-HT2C. For more information, please see the respective main articles of the individual subtypes: * 5-HT2A receptor * 5-HT2B receptor * 5-HT2C receptor See also * 5-HT1 receptor * 5-HT3 receptor * 5-HT4 receptor * 5-HT5 receptor * 5-HT6 receptor * 5-HT7 receptor * 5-HT2 antagonists References {{Serotonergics Serotonin receptors ... [...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] |
