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Phenylbiguanide (PBG) is a 5-HT3 agonist used to study the role of 5-HT3 receptors in the central nervous system. [1] It has been found to trigger dopamine release in the nucleus accumbens of rats. [ 2 ]
Biguanide (/ b aɪ ˈ ɡ w ɒ n aɪ d /) is the organic compound with the formula HN(C(NH)NH 2) 2. It is a colorless solid that dissolves in water to give a highly basic solution. It is a colorless solid that dissolves in water to give a highly basic solution.
[2] [5] DOHx has shown the highest affinity for the serotonin 5-HT 2A and 5-HT 2C receptors of any other assessed DOx drug in multiple studies. [2] [3] [6] [5] In one study, its affinities for the human serotonin 5-HT 2 receptors were 0.1 nM for the 5-HT 2A receptor, 30 nM for the 5-HT 2B receptor, and 0.7 nM for 5-HT 2C receptor.
[1] [2] [7] For comparison, the affinities of LSD and DOM in the same study were 6.31 nM and 18.6 nM, respectively. [7] DOSB substitutes for LSD in rodent drug discrimination tests, albeit much less potently than DOM ( ED 50 Tooltip median effective dose = 1.80 mg/kg versus 0.148 mg/kg, respectively; ~12-fold difference) and with only partial ...
2C-iBu is a highly potent and robustly efficacious serotonin 5-HT 2A receptor agonist. [4] Its EC 50 Tooltip half-maximal effective concentration values are 1.3 nM for calcium mobilization and 57.5 nM for β-arrestin-2 recruitment, whereas its E max Tooltip maximal efficacy values are 103% for calcium mobilization and 77% for β-arrestin-2 recruitment relative to serotonin. [4]
meta-Chlorophenylbiguanide (1-(3-Chlorophenylbiguanide, m-CPBG) is an allosteric agonist and modulator of the 5-HT 3 receptor [1] [2] [3] and an antagonist of the α 2A-adrenergic receptor. [4] It has anxiogenic , emetic and hypothermic effects in animal studies.
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In addition to the serotonin 5-HT 2A and 5-HT 2C receptors, BMB-A39a is a potent partial agonist of the serotonin 5-HT 1F and 5-HT 6 receptors. [3] Conversely, BMB-A39a shows minimal or negligible activity in activating the serotonin 5-HT 2B receptor ( E max < 20%) and does not activate other serotonin receptors .