Cho, Sung Jin published the artcileSelective 5-Hydroxytryptamine 2C Receptor Agonists Derived from the Lead Compound Tranylcypromine: Identification of Drugs with Antidepressant-Like Action, Formula: C8H6ClFO, the main research area is serotonin receptor 5HT2c agonist antidepressant tranylcypromine derivative SAR preparation.
We report here the design, synthesis, and pharmacol. properties of a series of compounds related to tranylcypromine (9), which itself was discovered as a lead compound in a high-throughput screening campaign. Starting from 9, which shows modest activity as a 5-HT2C agonist, a series of 1-aminomethyl-2-phenylcyclopropanes was investigated as 5-HT2C agonists through iterative structural modifications. Key pharmacophore feature of this new class of ligands is a 2-aminomethyl-trans-cyclopropyl side chain attached to a substituted benzene ring. Among the tested compounds, several were potent and efficacious 5-HT2C receptor agonists with selectivity over both 5-HT2A and 5-HT2B receptors in functional assays. The most promising compound is 37, with 120- and 14-fold selectivity over 5-HT2A and 5-HT2B, resp. (EC50 = 585, 65, and 4.8 nM at the 2A, 2B, and 2C subtypes, resp.). In animal studies, compound 37 (10-60 mg/kg) decreased immobility time in the mouse forced swim test.
Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 286474-59-7 belongs to class chlorides-buliding-blocks, name is 6-Chloro-2-fluoro-3-methylbenzaldehyde, and the molecular formula is C8H6ClFO, Formula: C8H6ClFO.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics