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.

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.

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.

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 is a potent corticotropin releasing factor (CRF) antagonist.

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

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.

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

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.

CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a K_i of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (K_i = >10 μM). CP 154526 has anxiolytic activities.

DMP 904 is a noncompetitive full corticotropin-releasing factor receptor (CRFR) antagonist. DMP 904 can inhibit CRF-stimulated adenylate cyclase activity and ACTH release. DMP 904 exhibits anti-depressant and anti-anxiety activity.

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).

NGD 98-2 hydrochloride is an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist

E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (K_i=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression.

BMS-763534 is a CRF1 antagonist that inhibits neurological disorders such as depression and anxiety..

BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer.

JNJ19567470 (R317573) is a selective, non-peptidergic CRF type 1 receptor (CRF1) antagonist. JNJ19567470 blocks NaLac-induced panic-like behaviour and cardiovascular responses. JNJ19567470 decreases regional glucose utilization in the amygdala, and attenuates anxiety responses.

(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) is a CRF antagonist. (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) prevents the IL-1a induced Luteinizing hormone (LH) inhibition.