Antalarmin (hydrochloride)

Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki 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[1][2][3].

Product Specifications

CAS Number

[220953-69-5]

UNSPSC

12352005

Target

CRFR

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/antalarmin-hydrochloride.html

Purity

99.87

Solubility

DMF : 20 mg/mL (ultrasonic; warming) |DMSO : 125 mg/mL (ultrasonic) |Ethanol : 14 mg/mL (ultrasonic; warming)

Smiles

CC1=C(N2C(C)=C(C)C3=C(N(CCCC)CC)N=C(C)N=C32)C(C)=CC(C)=C1.[H]Cl

Molecular Formula

C24H35ClN4

Molecular Weight

415.01

References & Citations

[1]Webster EL, et al. In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology. 1996 Dec;137 (12) :5747-50. doi: 10.1210/endo.137.12.8940412.|[2]Zorrilla EP, et al. Effects of antalarmin, a CRF type 1 receptor antagonist, on anxiety-like behavior and motor activation in the rat. Brain Res. 2002 Oct 18;952 (2) :188-99.|[3]Deak T, et al. The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress. Endocrinology. 1999 Jan;140 (1) :79-86. |[4]Cao J, et al. Human mast cells express corticotropin-releasing hormone (CRH) receptors and CRH leads to selective secretion of vascular endothelial growth factor. J Immunol. 2005 Jun 15;174 (12) :7665-75.