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CAS No. : 195055-03-9
MCE 国际站:R121919
产品活性:R121919 (NBI30775) 是一种高效的小分子 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。
研究领域:GPCR/G Protein
作用靶点:CRFR
In Vitro: R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2–5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
In Vivo: R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drug's intracellular targets.
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