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R121919 hydrochloride

CAS: 195055-66-4 F: C22H33ClN6 W: 416.99

R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 hydrochlorid
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Bioactivity R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats[1][2][3].
Invitro 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]。 0 --> R121919 hydrochloride 相关抗体:
In Vivo 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]。
Name R121919 hydrochloride
CAS 195055-66-4
Formula C22H33ClN6
Molar Mass 416.99
Transport Room temperature in continental US; may vary elsewhere.
Storage

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

Reference [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. [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. [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.