crf1 receptor

CP 316311 是一种特异性的 CRF1 receptor 拮抗剂，具有潜在的抗抑郁活性，可用于研究抑郁症。

Emicerfont is an antagonist of the corticotropin-releasing factor type 1 receptor (IC50: 66 nM).

CRF1 receptor antagonist-1 (Compound 2)为CRF1受体拮抗剂，适用于先天性肾上腺增生症(CAH)的研究领域。

Urotensin I acetate 是一种 CRF 样神经肽，可作为 CRF 受体激动剂，对 CHO 细胞中的人 CRF1、人 CRF2 和大鼠 CRF2α 受体的 pEC50 分别为 11.46、9.36 和 9.85，对 CHO 细胞的 Kis 分别为 0.4、1.8 和 5.7 nM hCRF1、rCRF2α 和 mCRF2β 受体。

Crinecerfont (SSR-125543) 是促肾上腺皮质激素释放因子 1 受体 (CRF1) 的特异性拮抗剂，可用于经典先天性肾上腺增生的研究。

NVS-CRF38 is an antagonist of corticotropin-releasing factor receptor 1 (CRF1).

Pexacerfont (BMS-562086) 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂，作用于人 CRF1 受体，IC50 为 6.1±0.6 nM。

R121919 (NBI30775) 是一种高效的促肾上腺皮质激素释放因子受体 1 （CRF1）小分子受体拮抗剂，具有抗抑郁和抗焦虑活性，抑制 CRF1 受体、 CRF2 受体和 CRF 结合蛋白。

Crinecerfont tosylate 是一种高效的口服CRF1 receptor拮抗剂，可用于先天性肾上腺增生 (CAH) 的研究。

CRF1 receptor antagonist

corticotropin-releasing factor1 (CRF1) receptor antagonist

corticotropin-releasing factor receptor 1 (CRF1) antagonist

BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addi

CP 154,526 is a selective CRF1 receptor antagonist (Ki = 2.7 nM). CP 154,526 blocks CRF-induced activation of adenylate cyclase and the HPA axis.

CRA1000, a CRF1 receptor antagonist, involved in the regulation of stress response.

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.

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).

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

Crinecerfont hydrochloride (SSR-125543) is a highly potent, orally active, non-peptide antagonist of the CRF1 receptor. It has demonstrated efficacy in the context of Classic congenital adrenal hyperplasia (CAH) research.

CP 376395 (CP-316311)是一种 CRF1受体选择性拮抗剂。

NBI-35965 is a CRF1 receptor antagonist.

Verucerfont (NBI77860) 是促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，作用于 CRF1(IC50:6.1 nM)，CRF2 (IC50>1000 nM)和 CRF-BP (IC50>1000 nM)。

K41498 TFA 是一种强选择性的CRF2 receptor 拮抗剂，其对人 CRF2α、CRF2β和 CRF1受体的Ki 值分别为 0.66 nM、0.62 nM 和425 nM。K41498 TFA 是 antisauvagine-30 (aSvg-30) 的类似物，可抑制 sauvagine 刺激的 cAMP 在 hCRF2α hCRF2β表达细胞中的积累。K41498 可用于低血压研究。

α-Helical CRF(9-41) TFA 是一种竞争性 CRF2受体拮抗剂，KB 约为 100 nM。α-Helical CRF(9-41) TFA 也是一种 CRF1受体的部分激动剂，EC50为 140 nM。