7-氯氯卡色林

7-氯氯卡色林，化学名(1R)-7,8-二氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂环庚三烯，是一种有机化合物，化学式为C11H13Cl2N。它是一种一种血清素5-HT2受体激动剂。它是食欲抑制剂和减肥药（Belviq）的结构类似物，最初于2005年被文献报道。Shah, J. H., Hindupur, R. M., & N Pati, H. (2015). Pharmacological and biological activities of benzazepines: An overview. Current Bioactive Compounds, 11(3), 170–188. https://doi.org/10.2174/1573407211666150910202200 "A series of 3-benzazepines was synthesized by Smith Jeffrey and Smith Brian [134]. These benzazepine act as modulators of 5-HT2C receptors and provide a number of potent and selective 5-HT2C receptor agonists. The functional activity of the compounds at the h5-HT2C (INI isoform), h5-HT2A, and h5-HT2B receptors is determined by measurement of [3H]-phosphoinositol turnover in transiently transfected HEK-293 cells. Lorcaserin (Fig. 17) acts as an anorectic and have serotonergic properties. It is a selective 5- HT2C receptor agonist and the drug showed reasonable selectivity for 5-HT2C over other related targets during in vivo and in vitro testing [135, 136]. It has shown 100x selectivity for 5-HT2C (EC50=39 nM) versus the closely related 5-HT2B (EC50=2380 nM) receptor, and 17x selectivity over the 5- HT2A (EC50= 553 nM) receptor. [...] When substituent at 7-position was added in lorcaserin, it increased 5-HT2C potency and even greatly increased in 5-HT2A and 5-HT2B receptor potencies resulting in reduced selectivity. [...]"

参考文献

Category:降食欲剂
Category:苯并氮杂䓬
Category:氯代芳烴
Category:对映纯药物