3-Substituted 1-methyl-3-benzazepin-2-ones as 5-HT2C receptor agonists?
RSC Advances Pub Date: 2015-10-19 DOI: 10.1039/C5RA17718A
Abstract
In search of potent and selective 5-HT2C receptor agonists, a series of novel 3-substituted 1-methyl-3-benzazepin-2-ones and 8-chloro-1-methyl-3-benzazepin-2-ones have been synthesized and evaluated for their 5-HT2C receptor agonistic potential. 5-HT2C receptor agonist activity was established with the despair swim test, plus maze test and the compounds' ability to decrease DA and 5-HT levels in rat brains similar to m-CPP. Selectivity was established with 5-HT2C mediated penile erection and hypophagic responses in the presence of RS-102221 (a selective 5-HT2C antagonist). The study established the selective 5-HT2C receptor agonist response of compounds 7, 12–14, 24, 30, and 38 which could act as potential lead molecules for the treatment of pathological conditions associated with 5-HT2C receptors.
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Journal Name:RSC Advances
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CAS no.: 89640-58-4