corticotropin-releasing factor receptor

Urocortin, human (Human urocortin I) is a 40 amino acid peptide which is closely related to corticotrophin-releasing factor (CRF).

Astressin acetate is an antagonist of corticotropin releasing factor (CRF) with low affinity for the CRF binding protein and high affinity for the cloned pituitary receptor(Ki = 2 nM).

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).

Urocortin II, mouse, is a selective and potent endogenous peptide agonist for the type-2 corticotropin-releasing factor (CRF2) receptor, displaying K_i values of 0.66 nM for CRFR2 and >100 nM for CRFR1, signifying its high specificity. It engages CRF2 receptors through mechanisms dependent on cAMP PKA and Ca2+ CaMKII. Additionally, Urocortin II, mouse is localized in specific regions of the central nervous system, influencing central neurons that process visceral sensory information and regulate autonomic functions [1] [2] [3].

Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide that primarily interacts with and activates the CRF receptor type 2 (CRF-R2), showing a specific distribution in the central nervous system and periphery. It selectively binds to type 2 CRF receptors with dissociation constants (Ki values) of 13.5 nM for mouse CRF2β, 21.7 nM for rat CRF2α, and >100 nM for human CRF1, indicating a strong preference for CRF-R2 over CRF1. Additionally, Urocortin III (human) plays a crucial role in the somatostatin-dependent negative feedback mechanism regulating the secretion of Insulin (human).

(Tyr0)-Urocortin, rat, serves as a high-affinity agonist for both corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2), demonstrating inhibitory binding constants (Ki) of 1-2 nM [1].

K 41498 is a selective peptide antagonist targeting both corticotropin-releasing factor receptor 2α (CRF2α) and CRF2β, demonstrating high affinity with Kis of 0.66 and 0.62 nM, respectively, in HEK293 cells expressing these human receptors. Its selectivity is evident as it exhibits a significantly reduced affinity for CRF1 receptor (Ki = 425 nM in HEK293 cells expressing the human CRF1 receptor). Additionally, K 41498, when administered intravenously at 1.84 µg/animal, effectively mitigates urocortin-induced hypotension in rats. Furthermore, its intrathecal delivery ranging from 0.075 to 0.5 µmol/animal significantly lowers the mechanical paw withdrawal threshold in a rat model, indicating its potential utility in managing nociception triggered by complete Freund's adjuvant.

Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor. Human urocortin II exhibits mild motor-suppressive effects and delayed anxiolytic-like effects,suggesting a time-depen

Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor.

Corticotropin-releasing factor receptor antagonist (Ki values are 17, 5 and 0.97 at human CRF1, rat CRF2α and mouse CRF2β receptors respectively).

Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells

Potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist (IC50 values are 1.3 and > 500 nM for CRF2 and CRF1 respectively). Antagonizes CRF2-mediated inhibition of gastric emptying.

Corticotropin-releasing factor (CRF) receptor agonist. Ki values are 9.4, 9.9, and 3.8 nM for inhibition of 125I-[D-Tyr1]astressin binding to hCRF-R1, rCRF-R2a and mCRF-R2b respectively.

Potent and selective corticotropin releasing factor receptor-1 (CRF1) agonist (Ki values are 1.5 and 224 nM for CRF1 and CRF2 receptors respectively). Increases ACTH levels and increases faecal pellet output in vivo following i.p. administration.