|
2C-BI-8
2C-BI-8, also known as 2,5-dimethoxy-4-(4-methoxyphenyl)phenethylamine or as 4′-methoxy-2C-Ph, is a serotonin receptor agonist of the phenethylamine and 2C families. It is the derivative of 2C-Ph (2C-BI-1) with a methoxy group at the 4 position of the added phenyl ring. The drug binds to and/or activates the serotonin 5-HT2 receptors. At the human serotonin 5-HT2A receptor, its affinity (Ki) is 19nM, activational potency () is 37nM, and intrinsic activity () is 40%. These were among the most potent and efficacious in a series of evaluated 2C-Ph derivatives (2C-BI compounds) that included 2C-BI-8. However, 2C-BI-8's activational potency was about 18-fold lower than that of 2C-B and its efficacy was less than half of that of 2C-B. The drug also interacts with certain other monoamine receptors and has been assessed at the monoamine transporters. It may have the potential to produce psychedelic effects in humans. 2C-BI-8 was first described in the scientific literature by Danie ... [...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 phenethylamine and 2C families that was developed by Daniel Trachsel and David E. Nichols and colleagues. The drug's affinity (Ki) for the rat serotonin 5-HT2A receptor was 778nM. It was said to be an 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, 5-HT2B, and 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 potent and high-efficacy partial agonist of the human trace amine-associated receptor 1 (TAAR1) ( = 580nM, = 82%). Besides 2C-Ph itself, a variety of derivatives of 2C-Ph with substituents on the 4-position phenyl ring have been synthesized and studied by Trachsel and colle ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-T-33
2C-T-33, also known as 4-(3-methoxybenzylthio)-2,5-dimethoxyphenethylamine, is a serotonin receptor agonist of the phenethylamine and 2C families. It was first synthesized and described by Daniel Trachsel in 2003. The drug is not known to have ever been tested in humans and its active human doses have not been reported. Pharmacology 2C-T-33 shows high affinity for the serotonin 5-HT2A receptor (Ki = 1.7nM) and to a much lesser extent for the serotonin 5-HT2C receptor (Ki = 75nM; 44-fold lower than for 5-HT2A). In terms of serotonin 5-HT2A receptor activation, its is 26nM and its is 40%. Hence, 2C-T-33 acts as a low-efficacy partial agonist of the serotonin 5-HT2A receptor. The drug shows higher affinity for the serotonin 5-HT2A receptor but much lower potency and efficacy in activating the receptor compared to 2C-T or 2C-B (which had values of Ki = 6.9–49nM, = 2.0–2.1nM, and = 75–92%). In contrast to most other 2C drugs and serotonergic psychedelics, 2C-T-33 appear ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Daniel Trachsel
Daniel Trachsel is a Swiss people, Swiss chemist who studies psychedelic drug, psychedelics and entactogens. He has developed and published on a large number of novel psychedelic and entactogen chemical compound, compounds, including their psychoactive drug, psychoactive effects. This has been in a manner similar to that of the psychedelic chemist Alexander Shulgin, which has caused Trachsel to sometimes be referred to as the "German Shulgin". However, unlike Shulgin, Trachsel has distanced himself from any personal self-experimentation, self-experiments. According to Hamilton Morris and Nick Cozzi in mid-2023, Trachel's book ''Phenethylamine: von der Struktur zur Funktion'' (''Phenethylamines: From Structure to Function'') is in the process of being translated into English. It is being independently translated by the Alexander Shulgin Research Institute (ASRI), with tentative publication by Transform Press, and also by chemist David Carlson. Compounds Compounds that were first k ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Modulator
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission. The serotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamate, 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, nausea, sleep, and thermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, includin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Transporter
Monoamine transporters (MATs) are proteins that function as integral Cell membrane, plasma-membrane Neurotransmitter transporter, transporters to regulate concentrations of extracellular monoamine neurotransmitters. The three major classes are serotonin transporters (SERTs), dopamine transporters (DATs), and norepinephrine transporters (NETs) and are responsible for the reuptake of their associated amine neurotransmitters (serotonin, dopamine, and norepinephrine). MATs are located just outside the synaptic cleft (peri-synaptically), transporting monoamine transmitter overflow from the synaptic cleft back to the cytoplasm of the pre-synaptic neuron. MAT regulation generally occurs through protein phosphorylation and post-translational modification. Due to their significance in neuronal signaling, MATs are commonly associated with drugs used to Psychiatric medication, treat mental disorders as well as recreational drugs. Compounds targeting MATs range from medications such as the wi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2B Agonists
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and v ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,5-Dimethoxy-4-benzylamphetamine
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, also known as 4-benzyloxy-3,5-dimethoxyamphet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 phenethylamine and 2C families that was developed by Daniel Trachsel and David E. Nichols and colleagues. The drug's affinity (Ki) ... * DOHx References External links DOPhPr - Isomer Design 5-HT2A agoni ... [...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 Benzscaline (BZ), also known as 4-benzyloxy-3,5-dimethoxyphenethylamine (4-Bzl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
