crfr1;crfr1;crfr1

Antisauvagine-30 TFA (aSvg-30 TFA) is a highly selective and competitive antagonist of CRF2 receptor peptidic. It shows a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively.

NBI 35965 methanesulfonate  is a CRF1 antagonist.

NBI-34041 is an effective and high-affinity CRF1 receptor antagonist that effectively reduces endocrine responses to CRF(1) receptor-mediated pharmacological and behavioral challenges.

High affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable. Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216 |Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 180 215 PMID:15696320 |Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID:12538845 |Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID:12093593

NBI-27914 是一种有效的、选择性的 CRFR1 拮抗剂。其中 CRF 受体 CRFR1 和 CRFR2 是 G 蛋白偶联受体超家族的成员。

Antisauvagine-30 TFA (aSvg-30 TFA) 是有效的、高度选择性的、竞争性的CRF2受体的多肽拮抗剂。Antisauvagine-30 TFA 对 mCRFR2β 和CRFR1的Kd 值分别为1.4 nM 和150 nM。

Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂，对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP PKA 和 Ca2+ CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达，并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。

NBI 35965 hydrochloride 是一种选择性、口服活性、能穿过血脑屏障的促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，Ki 值为 4 nM，pKi 值为 8.5，并且不抑制 CRF2。NBI 35965 hydrochloride 可减少体内 CRF 或应激诱导的促肾上腺皮质激素 (ACTH) 生成，pIC50 值分别为 7.1 和 6.9，具有抗焦虑作用。