crf1 receptor

CP 316311 is a specific CRF1 receptor antagonist with potential antidepressant activity and may be used in the study of depression.

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

CRF1 Receptor Antagonist-1 (Compound 2), a CRF1 receptor antagonist, is utilized in research pertaining to congenital adrenal hyperplasia (CAH) [1].

Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).

R121919 (NBI30775) is a potent small molecule antagonist of the adrenocorticotropic hormone-releasing factor receptor 1 (CRF1), demonstrating antidepressant and anxiolytic activity, and inhibiting the CRF1 receptor, CRF2 receptor, and CRF-binding proteins.

corticotropin-releasing factor1 (CRF1) receptor antagonist

Crinecerfont (SSR-125543) is a selective antagonist of corticotropin-releasing factor 1 receptor (CRF1) and can be used in studies about Classic congenital adrenal hyperplasia.

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

Crinecerfont tosylate is an effective oral CRF1 receptor antagonist. It is applicable to studies involving congenital adrenal hyperplasia (CAH).

AAG561 is a corticotropin-releasing factor receptor 1 (CRF1) antagonist. It is useful for researching potential emotional dysregulation associated with psychiatric disorders or mental illnesses.

CP 154526 hydrochloride is a blood-brain barrier-penetrant, selective CRF1 (corticotropin-releasing factor receptor 1) antagonist (Ki = 2.7 nM) exhibiting thousands of times greater selectivity for CRF1 over CRF2, with anxiolytic and antidepressant activities.

corticotropin-releasing factor receptor 1 (CRF1) antagonist

BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM) that inhibits CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). It is also efficacious in the Defensive Withdrawal model of anxiety in rats and has low in vivo clearance [Cl = 17 mL/min/kg, t½ = 7.8 h].

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, demonstrating efficacy in Classic congenital adrenal hyperplasia (CAH) research.

CP 376395 (CP-316311) is an effective and specific Corticotropin-releasing factor 1 (CRF1) receptor antagonist.

NBI-35965 is a CRF1 receptor antagonist.

Verucerfont (NBI77860) is an antagonist of corticotropin-releasing factor receptor 1 (CRF1) .

K41498 TFA, an analog of antisauvagine-30 (aSvg-30), is a potent and highly selective antagonist of CRF2 receptors, exhibiting K i values of 0.66 nM, 0.62 nM, and 425 nM for human CRF 2α, CRF 2β, and CRF 1 receptors, respectively. This compound effectively inhibits sauvagine-stimulated cAMP accumulation in cells expressing hCRF 2α and hCRF 2β. It is utilized in studies investigating hypotension [1].

α-Helical CRF(9-41) TFA acts as a competitive antagonist for the CRF2 receptor, with a binding constant (K B) of approximately 100 nM, and serves as a partial agonist for the CRF1 receptor, exhibiting a half-maximal effective concentration (EC 50) of 140 nM [1] [2].