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4-PhPr-2,5-DMA
4-(3-Phenylpropyl)-2,5-dimethoxyamphetamine (DOPP or DOPhPr), also known as 4-PhPr-2,5-DMA, is a serotonin receptor modulator of the phenethylamine, amphetamine, and DOx families. It shows high affinity for both the serotonin 5-HT2A and 5-HT2C receptors and acts as a weak partial agonist or antagonist of the serotonin 5-HT2A receptor. The drug has lower affinity for the serotonin 5-HT2A receptor than its closely related positional isomer 4-PhPr-3,5-DMA. This is an apparent reversal of the usual situation with DOx and related drugs in which the 2,5-dimethoxy pattern is optimal for serotonin 5-HT2A receptor interactions. See also * DOBz * 2C-T-27 * 2C-Ph 2C-Ph, also known as 2C-BI-1 or as 2,5-dimethoxy-4-phenylphenethylamine, is a serotonin receptor modulator of the substituted phenethylamine, phenethylamine and 2C drugs, 2C families that was developed by Daniel Trachsel and David E. Nichols and ... * DOHx References External links DOPhPr - Isomer Design 5-HT2A ago ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-Ph
2C-Ph, also known as 2C-BI-1 or as 2,5-dimethoxy-4-phenylphenethylamine, is a serotonin receptor modulator of the substituted phenethylamine, phenethylamine and 2C drugs, 2C families that was developed by Daniel Trachsel and David E. Nichols and colleagues. The drug's affinity (pharmacology), affinity (Ki) for the rat serotonin 5-HT2A receptor, 5-HT2A receptor was 778nM. It was said to be an receptor antagonist, antagonist of this receptor. In a subsequent study, 2C-Ph was a weak partial agonist of the human serotonin 5-HT2A receptor (Ki = 630nM, = 1,596nM, = 23%). The drug also shows affinity for the serotonin 5-HT1A receptor, 5-HT1A, 5-HT2B receptor, 5-HT2B, and 5-HT2C receptor, 5-HT2C receptors, but did not activate the serotonin 5-HT2B receptor. In addition, it interacted with other monoamine receptors, with the monoamine transporters, and was a potency (pharmacology), potent and high-efficacy partial agonist of the human trace amine-associated receptor 1 (TAAR1) ( = 580nM, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOBz
2,5-Dimethoxy-4-benzylamphetamine (DOBz or DOBN) is a serotonin 5-HT2 receptor modulator of the amphetamine and DOx families. It is the DOx derivative with a benzyl ring at the 4 position. The drug's affinities (Ki) for the human serotonin 5-HT2 receptors have been found to be 0.40nM for the serotonin 5-HT2A receptor, 24.5 to 35.0nM for the serotonin 5-HT2B receptor, and 1.0nM for the serotonin 5-HT2C receptor. Its affinities for the serotonin 5-HT2 receptors are very similar to those of DOB. The drug has been assessed and found to act as a silent antagonist of the serotonin 5-HT2B receptor ( = 0%). In rodent drug discrimination tests, DOBz neither antagonized nor generalized to the stimulus of DOM. Higher doses produced behavioral disruption however. DOBz was first described in the scientific literature by Richard Glennon and colleagues in 1989. See also * 2C-Ph * 4-PhPr-2,5-DMA * 2C-T-27 * Benzscaline (BZ) * 3C-BZ 3C-BZ (4-benzyloxy-3,5-dimethoxyamphetamine) is a le ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-PhPr-3,5-DMA
4-PhPr-3,5-DMA, also known as 4-(3-phenylpropyl)-3,5-dimethoxyamphetamine, is a serotonin receptor modulator of the phenethylamine and amphetamine families. It is structurally related to the DOx drugs but has one of its methoxy groups in the 3 position instead of 2 position on the phenyl ring and has a bulky substitution at the 4 position of the phenyl ring. The affinities (Ki) of 4-PhPr-3,5-DMA for the serotonin 5-HT2 receptors have been reported to be 4nM for the serotonin 5-HT2A receptor and 40nM for the serotonin 5-HT2C receptor, with approximately 10-fold selectivity for the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor. Its affinities for the serotonin 5-HT2A and 5-HT2C receptors in the study were approximately 8-fold and 1.6-fold higher than those of DOB, respectively. The drug was a full agonist of the serotonin 5-HT2A receptor in terms of phosphatidylinositol (PI) hydrolysis ( = 109% relative to serotonin). However, in the presence of the serotonin 5 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the Central nervous system, central and peripheral nervous systems. They mediate both Neurotransmitter#Excitatory and inhibitory, excitatory and inhibitory Synaptic transmission, neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural Ligand (biochemistry), ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamic acid, glutamate, gamma-Aminobutyric acid, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, Mood (psychology), mood, nausea, sleep, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
DOx (psychedelics)
4-Substituted-2,5-dimethoxyamphetamines (DO''x'') is a chemical class of substituted amphetamine derivatives featuring methoxy groups at the 2- and 5- positions of the phenyl ring, and a substituent such as alkyl or halogen at the 4- position of the phenyl ring. Most compounds of this class are potent and long-lasting psychedelic drugs, and act as highly selective 5-HT2A, 5-HT2B, and 5-HT2C receptor partial agonists. A few bulkier derivatives such as DOAM have similarly high binding affinity for 5-HT2 receptors but instead act as antagonists, and so do not produce psychedelic effects though they retain amphetamine-like stimulant effects. DOx derivatives The DO''x'' family includes the following members: Related compounds A number of additional compounds are known with alternative substitutions: See also * 2Cs, 25-NB * Substituted amphetamines * Substituted benzofurans * Substituted cathinones * Substituted methylenedioxyphenethylamines * Substituted phenethylamines * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A 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] |
DOHx
2,5-Dimethoxy-4-hexylamphetamine (DOHx or DOHE) is a non-hallucinogenic serotonin receptor modulator of the phenethylamine, amphetamine, and DOx families. Pharmacology DOHx has shown the highest affinity for the serotonin 5-HT2A and 5-HT2C receptors of any other assessed DOx drug in multiple studies. In one study, its affinities for the human serotonin 5-HT2 receptors were 0.1nM for the 5-HT2A receptor, 30nM for the 5-HT2B receptor, and 0.7nM for 5-HT2C receptor. In the case of the serotonin 5-HT2A receptor, this was 6- to 14-fold higher than DOB, DOI, and DOC and was 9-fold higher than DOPR. In another study, DOHx showed 25-fold higher affinity for the serotonin 5-HT2A receptor than DOM or DOET, 23- to 28-fold higher affinity than DOPR and DOBU, and 2.8-fold higher affinity than DOAM. Conversely, it showed only slightly higher or roughly the same affinity for the receptor relative to DOCT (2.5nM vs. 3.0nM, respectively). In contrast to many other DOx drugs, DOHx, as wel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-T-27
2C-T-27, also known as 4-benzylthio-2,5-dimethoxyphenethylamine, is a serotonin 5-HT2A receptor agonist and serotonergic psychedelic of the phenethylamine and 2C families. It was first synthesized and described by Daniel Trachsel in 2003. In addition to the serotonin 5-HT2A receptor, 2C-T-27 interacts with the serotonin 5-HT2C receptor. It showed higher affinity for the serotonin 5-HT2A receptor than any other 2C drug (Ki = 1.6nM), but its activational potency and efficacy were among the lowest ( = 26nM; = 27%). The drug produces the head-twitch response (HTR), a behavioral proxy of psychedelic effects, in rodents. However, the HTR induced by 2C-T-27 is relatively weak. 2C-T-27 has been reported to produce hallucinogenic effects in humans. Its dosage was reported by Trachsel to be 80mg or more orally and no duration was listed. See also * 2C-T-33 * 2C-T-8 * Aleph-6 * 3C-BZ * Benzscaline (BZ) * 2C-Ph 2C-Ph, also known as 2C-BI-1 or as 2,5-dimethoxy-4-phenylphenethyla ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Positional Isomer
In chemistry, a structural isomer (or constitutional isomer in the IUPAC nomenclature) of a compound is another compound whose molecule has the same number of atoms of each element, but with logically distinct bonds between them. The term metamer was formerly used for the same concept. For example, butanol , methyl propyl ether , and diethyl ether have the same molecular formula but are three distinct structural isomers. The concept applies also to polyatomic ions with the same total charge. A classical example is the cyanate ion and the fulminate ion . It is also extended to ionic compounds, so that (for example) ammonium cyanate and urea are considered structural isomers,William F. Bynum, E. Janet Browne, Roy Porter (2014): ''Dictionary of the History of Science''. 530 pages. and so are methylammonium formate and ammonium acetate . Structural isomerism is the most radical type of isomerism. It is opposed to stereoisomerism, in which the atoms and bonding schem ... [...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 epit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Modulator
A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activity in a positive, negative, or neutral direction with varying degrees of efficacy. Categories of these modulators include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, orthosteric modulators, and allosteric modulators, Examples of receptor modulators in modern medicine include CFTR modulators, selective androgen receptor modulators (SARMs), and muscarinic ACh receptor modulators. = General Description = Currently, receptor modulators are categorized in the Agonist, Partial Agonist, Selective Tissue Modulators, Antagonist, and Inverse Agonist categories in terms of the affect they cause. They are further divided into Orthosteric or Allosteric Modulators according to how they effect said ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
