一种高效的小分子 CRF1 受体拮抗剂。对于 CRF1 受体的 Ki 值为 2 至 5 nM,对 CRF2 受体,CRF 结合蛋白或 70 种其它受体类型的活性弱超过 1000 倍。
R121919 is a CRF1 receptor antagonist. R121919 attenuates the severity of precipitated morphine. Treatment with R121919 improves sleep-EEG in patients with depression. R121919 attenuates stress-elicited sleep disturbances in rats, particularly in those with high innate anxiety.