CRFR Antagonist

Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a K_i of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome.

R121919 (NBI30775) is a potent and selective CRF1R antagonist with a K_i of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats.

NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a K_i value of 3.4 nM for the human receptor. NBI 30545 inhibits CRF-stimulated intracellular cAMP accumulation and ACTH release. NBI 30545 can be used in the research of depression, anxiety disorders and stress-related diseases.

CRF1 receptor antagonist-2 is an orally active, blood-brain barrier permeable CRF1 receptor antagonist, with an IC₅₀ of 4 nM in CHO-K1 cell membranes and an IC₅₀ of 7 nM in rat brain cell membranes. CRF1 receptor antagonist-2 exerts anxiolytic effects in swim stress-loaded rats. CRF1 receptor antagonist-2 can be used in studies related to stress-induced anxiety.

NBI-27914 is a highly selective, high-affinity non-peptide competitive antagonist of human corticotropin-releasing factor receptor 1 (CRFR1). NBI-27914 primarily binds to the His199 and Met276 sites in the transmembrane domain of the receptor.

Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a K_i of 2.7 nM. Antalarmin can pass through the blood–brain barrier.

Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.

Astressin is a potent corticotropin releasing factor (CRF) antagonist.

Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC₅₀=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.

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

CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.

Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC₅₀s of ~6.1, >1000 and >1000?nM for CRF1, CRF2, and CRF-BP, respectively.

Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF₂ receptor antagonist with K_d values of 1.4 nM and 153.6 nM for mouse CRF_2β and rat CRF₁ receptors, respectively.

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

K41498 is a highly selective CRF 2 receptor antagonist, with a K_i of 0.66 nM for human CRF2α receptor and a K_i of 0.62 nM for human CRF2β receptor. K41498 inhibits cAMP accumulation in cells expressing CRF2. K41498 antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues.

DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression.

NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a K_i value of 1.7 nM.

NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a K_i value of 4 nM and a pK_i value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC₅₀ values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects.

Emicerfont is a corticotropin-releasing factor type 1 (CRF₁) receptor antagonist with an IC₅₀ of 66 nM.

NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.