3-Substituted 1-methyl-3-benzazepin-2-ones as 5-HT2C receptor agonists

Abstract

In search of potent and selective 5-HT_2C 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-HT_2C receptor agonistic potential. 5-HT_2C 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-HT_2C mediated penile erection and hypophagic responses in the presence of RS-102221 (a selective 5-HT_2C antagonist). The study established the selective 5-HT_2C 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-HT_2C receptors.