R121919 hydrochloride  (Synonyms: NBI30775 hydrochloride)

R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a K_i of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats^[1][2][3].

R121919 hydrochloride 是一种强效小分子 CRF1 受体拮抗剂，对 CRF1 受体具有高亲和力，但对 CRF2 受体、CRF 结合蛋白或 70 种其他受体类型的活性较弱 1000 倍以上^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

R121919 (NBI30775) hydrochloride 剂量依赖性地降低大鼠肾上腺皮质激素和皮质酮 (HY-B1618) 对束缚应激的反应。R121919 剂量为 10 mg/kg 时，血浆肾上腺皮质激素和皮质酮的峰值浓度分别为 9% 和 25%^[1]。
R121919 hydrochloride 可降低大剂量小鼠的焦虑水平-响应曲线^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

416.99

C₂₂H₃₃ClN₆

195055-66-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80.  [Content Brief]

  [2]. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.  [Content Brief]

  [3]. Gutman DA, et al. Behavioral effects of the CRF1 recepator antagonist R121919 in rats selectively bred for high and low activity in the swim test. Psychoneuroendocrinology. 2008 Sep;33(8):1093-101.  [Content Brief]