SB-269970

SB-269970 is a potent and selective small molecule antagonist of the serotonin receptor 7 (5-HT7), developed by GlaxoSmithKline/SmithKline Beecham for research purposes. It acts as either a selective antagonist or inverse agonist at the 5-HT7 receptor with high affinity (pKi ~8.9 for 5-HT7A), and shows much lower activity at other serotonin receptors, confirming its selectivity[1][3][4]. In animal studies, it has demonstrated anxiolytic-, antidepressant-, anticonvulsant-, and procognitive-like effects without significant motor side effects[6][8][10]. The compound is brain penetrant and used primarily to study the role of the 5-HT7 receptor in neuropsychiatric disorders such as anxiety, depression, epilepsy/seizures, cognitive flexibility/impairment, and potentially diabetes-related beta cell protection[6][8][9]. No clinical development or approval for human therapeutic use has been reported; all data are preclinical.

Other names

3-[[(2R)-2-[2-(4-methyl-1-piperidinyl)ethyl]-1-pyrrolidinyl]sulfonyl]phenol(2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine hydrochloride