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Org 12,962
ORG-12962 is a pyridinylpiperazine drug developed by Organon, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity at 5-HT2C and lowest at 5-HT2B subtypes. It was developed as a potential anti-anxiety drug, but was discontinued from human trials after tests in a public speaking challenge showed that its anti-anxiety effects were accompanied by side effects such as dizziness and a "spacey" feeling, which were attributed to poor selectivity ''in vivo'' over the hallucinogenic 5-HT2A receptor. Synthesis Note that patent serves to deliver 1- -chloro-5-(trifluoromethyl)pyridin-2-yliperazine 32834-59-4 although patent is correct oneCID:9796408 Hence, ORG-12962, would need 2,6-Dichloro-3-(trifluoromethyl)pyridine 5304-75-1 2,3-dichloro-5-trifluoromethylpyridine 9045-84-7 See also * 2C-B-PP * 2,3-Dichlorophenylpiperazine * 3-Chloro-4-fluorophenylpiperazine 3-Chloro-4-fluorophenylpiperazine (3,4-CFP, Kleferein) is a psychoactive d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyridinylpiperazine
1-(2-Pyridinyl)piperazine is a chemical compound and piperazine derivative. Some derivatives of this substance are known to act as potent and selective α2-adrenergic receptor antagonists, such as 1-(3-fluoro-2-pyridinyl)piperazine. A few pyridinylpiperazine derivatives are drugs, including: * ABT-724 AR234960* Azaperol 804-05-9* Azaperone — antipsychotic * Atevirdine — antiretroviral BRN 0563047 9215-20-2"''Stimulating dopaminerginic activity''": Journal Ref (Cmp XVIII): * CP-226,269 * Delavirdine — antiretroviral * Mirtazapine — antidepressant MLS1547 15698-36-3Revenast 5673-87-6UMB38ref> XH-148 See also * Diphenylmethylpiperazine * Benzylpiperazine * Phenylpiperazine 1-Phenylpiperazine is a simple chemical compound featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class. List phenylpiperazine derivativesAlpe ... * Pyrimidinylpiperazine References P ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5HT2A 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 otherwise ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperazines
Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and some are used in scientific research. List of substituted piperazines Benzylpiperazines File:Benzylpiperazine.svg, 1-Benzylpiperazine File:MBZP.svg, 1-Methyl-4-benzylpiperazine File:DBZP.svg, 1,4-Dibenzylpiperazine File:MDBZP.svg, 3,4-Methylenedioxy-1-benzylpiperazine File:2C-B-BZP.svg, 4-Bromo-2,5-dimethoxy-1-benzylpiperazine File:Methoxypiperamide.png, Methoxypiperamide File:Sunifiram.svg , Sunifiram File:3-Methylbenzylpiperazine structure.png, 3-Methylbenzylpiperazine * 1-Benzylpiperazine (BZP) * 1-Methyl-4-benzylpiperazine (MBZP) * 1,4-Dibenzylpiperazine (DBZP) * 3,4-Methylenedioxy-1-benzylpiperazine (MDBZP) * 4-Bromo-2,5-dimethoxy-1-benzylpiperazine (2C-B-BZP) * Methoxypiperamide (MeOP, MEXP) ((4-methoxyphenyl)(4-methylpiperazin-1-yl)methanone) * Sunifiram (1-benzoyl-4-propanoylpiperazine) * 3-Methylbenzylpiperazine (3-MeBZP) Befuraline, ... [...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] |
Quipazine
Quipazine is a serotonergic drug of the piperazine group which is used in scientific research. It was originally intended as an antidepressant but never developed for medical use. Pharmacology Pharmacodynamics Quipazine is a serotonin reuptake inhibitor, and also a moderately selective serotonin receptor agonist, binding to a range of different serotonin receptors, but particularly to the 5-HT2A and 5-HT3 subtypes. Quipazine produces a head-twitch response and other psychedelic-consistent effects in animal studies including in mice, rats, and monkeys. However, it failed to produce psychedelic effects in humans at a dose of 25 mg, which was the highest dose tested due to 5-HT3 mediated side effects of nausea and gastrointestinal discomfort. However Alexander Shulgin claimed that a fully effective psychedelic dose could be reached by blocking 5-HT3 receptors using a 5-HT3 antagonist. Chemistry Quipazine is synthesized by reacting 2-chloroquinoline with piperazine. S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ORG-37684
ORG-37684 is a drug developed by Organon, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity at 5-HT2C and lowest at 5-HT2B subtypes. It has anorectic effects in animal studies and has been researched as a potential weight loss drug for use in humans. See also * ORG-12962 * Quipazine Quipazine is a serotonergic drug of the piperazine group which is used in scientific research. It was originally intended as an antidepressant but never developed for medical use. Pharmacology Pharmacodynamics Quipazine is a serotonin reuptake ... References Serotonin receptor agonists Indanes Phenol ethers Pyrrolidines {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CPD-1
CPD-1 (LS-193743) is a drug with a benzofuranyl piperazine structure, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity and full agonist efficacy at the 5-HT2C subtype, and lower affinity and partial agonist action at the 5-HT2A and 5-HT2B subtypes. See also * 2,3-Dichlorophenylpiperazine * 3-Chloro-4-fluorophenylpiperazine * 2C-B-PP * ORG-12962 * TFMFly * TFMPP 3-Trifluoromethylphenylpiperazine (TFMPP) is a recreational drug Recreational drug use indicates the use of one or more psychoactive drugs to induce an altered state of consciousness either for pleasure or for some other casual purpose or pas ... References Serotonin receptor agonists Trifluoromethyl compounds Benzofurans N-(2-methoxyphenyl)piperazines {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-Chloro-4-fluorophenylpiperazine
3-Chloro-4-fluorophenylpiperazine (3,4-CFP, Kleferein) is a psychoactive drug of the phenylpiperazine class. It has been sold as a designer drug, first being identified in Poland in 2019. See also * 2,3-Dichlorophenylpiperazine * 2C-B-PP * 3C-PEP * CPD-1 CPD-1 (LS-193743) is a drug with a benzofuranyl piperazine structure, which acts as a potent and selective agonist for the 5-HT2 receptor family, with highest affinity and full agonist efficacy at the 5-HT2C subtype, and lower affinity and pa ... * Org 12962 References {{DEFAULTSORT:Chloro-4-fluorophenylpiperazine, 3- Chlorobenzenes Phenylpiperazines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,3-Dichlorophenylpiperazine
2,3-Dichlorophenylpiperazine (2,3-DCPP or DCPP) is a chemical compound from the phenylpiperazine family. It is both a precursor in the synthesis of aripiprazole and one of its metabolites. It is unclear whether 2,3-DCPP is pharmacologically active as a serotonin receptor agonist similar to its close analogue 3-chlorophenylpiperazine (''m''CPP), though it has been shown to act as a partial agonist of the dopamine D2 and D3 receptors. Legality 2,3-DCPP has been made illegal in Japan and Hungary after having been identified in seized designer drug samples. List of derivatives #Aripiprazole #Cariprazine #BAK 2-66 # Brilaroxazine (formally RP-5063) #FAUC-365 74432-66-1#CJB-090 2xHCl 95584-40-0#NGB 2849 89061-11-8#NGB 2904 Fb: 89061-11-8HCl: 89060-98-8br>PG-010372xHCl: 75599-62-9#PG648Aripiptranyl(Abilifarnate) #PGX-2000001 #So-calleR-22ref name="pmid22632094"/> #So-calleJJC 7−065ref name="pmid22632094"/>R-PG-648 Positional Isomer The positional isomer 3,4-dichlorophenylpipe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-B-PP
2,5-dimethoxy-4-bromophenylpiperazine (2C-B-PP) is a drug of the phenylpiperazine class. It acts as an agonist at serotonin receptors, and in studies on rats substituted for the psychedelic amphetamine derivative DOM with around 1/10 the potency but similar rates of stimulus-appropriate responding at the highest dose. See also * 2C-B-aminorex * 2C-B-BZP * 3-Chloro-4-fluorophenylpiperazine * CPD-1 * ORG-12962 * Quipazine * Substituted piperazine Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and some are used in scientific research. List of substituted piperazines Benzylpiperazines File:Benzylpiperazine.svg, 1- ... References {{Piperazines Bromoarenes Phenylpiperazines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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