Antalarmin hydrochloride

Names

[ CAS No. ]:
220953-69-5

[ Name ]:
Antalarmin hydrochloride

[Synonym ]:
7H-Pyrrolo[2,3-d]pyrimidin-4-amine, N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)-, hydrochloride (1:1)
N-Butyl-N-ethyl-7-mesityl-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride (1:1)
N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine,hydrochloride

Biological Activity

[Description]:

Antalarmin (hydrochloride) is a 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].

[Related Catalog]:

Research Areas >> Endocrinology

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₃₅ClN₄

[ Molecular Weight ]:
415.014

[ Exact Mass ]:
414.255035

[ PSA ]:
33.95000

[ LogP ]:
6.69930

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
22-24/25

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Increased CRF signalling in a ventral tegmental area-interpeduncular nucleus-medial habenula circuit induces anxiety during nicotine withdrawal.

Nat. Commun. 6 , 6770, (2015)

Increased anxiety is a prominent withdrawal symptom in abstinent smokers, yet the neuroanatomical and molecular bases underlying it are unclear. Here we show that withdrawal-induced anxiety increases ...

CRF-amplified neuronal TLR4/MCP-1 signaling regulates alcohol self-administration.

Neuropsychopharmacology 40(6) , 1549-59, (2015)

Alcohol dependence is a complex disorder that initiates with episodes of excessive alcohol drinking known as binge drinking. It has a 50-60% risk contribution from inherited susceptibility genes; howe...

Stress during a critical postnatal period induces region-specific structural abnormalities and dysfunction of the prefrontal cortex via CRF1.

Neuropsychopharmacology 40(5) , 1203-15, (2015)

During the early postnatal period, environmental influences play a pivotal role in shaping the development of the neocortex, including the prefrontal cortex (PFC) that is crucial for working memory an...