Antalarmin

Modify Date: 2023-01-17 19:11:26

Antalarmin structure	Common Name	Antalarmin
	CAS Number	157284-96-3	Molecular Weight	378.55400
	Density	1.05g/cm3	Boiling Point	437.2ºC at 760mmHg
	Molecular Formula	C₂₄H₃₄N₄	Melting Point	N/A
	MSDS	N/A	Flash Point	218.2ºC

Use of Antalarmin

Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier[1][2][3].

Name	N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
Synonym	More Synonyms

Description	Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier[1][2][3].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> CRFR Research Areas >> Neurological Disease
Target	Ki: 2.7 nM (CRHR1)[3]
In Vitro	Antalarmin 通过 cAMP/PKA 信号通路抑制促肾上腺皮质激素释放因子 (CRF) 对 Aβ1-42 水平的影响[2]。 Western Blot Analysis[2] Cell Line: Primary hippocampal neurons derived from Tg2576 mice Concentration: 100 nM Incubation Time: 48 h Result: Blocked CRF-induced increases in PKAIIβ levels.
In Vivo	Antalarmin (10 mg/kg; i.p.; daily for 4 weeks) 可以改善小鼠的慢性轻度应激 (CMS) 诱导的变化[1]。 Antalarmin (20 mg/kg; i.p.; daily for 7 days) 显著降低亚急性应激 Tg2576 小鼠中 Aβ1-42 水平[2]。 Animal Model: BALB/cByJIco male mice, chronic mild stress model[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection, daily for 4 weeks Result: Induced a significant improvement of mice physical state. Induced a nonsignificant decrease of the lit box (TLB) and activity when compared to controls.
References	[1]. Ducottet C, et al. Effects of the selective nonpeptide corticotropin-releasing factor receptor 1 antagonist antalarmin in the chronic mild stress model of depression in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Jun;27(4):625-31. [2]. Dong H, et al. Effects of corticotrophin-releasing factor receptor 1 antagonists on amyloid-β and behavior in Tg2576 mice. Psychopharmacology (Berl). 2014 Dec;231(24):4711-22. [3]. Zorrilla EP, et al. Urocortin shares the memory modulating effects of corticotropin-releasing factor (CRF): mediation by CRF1 receptors. Brain Res. 2002 Oct 18;952(2):200-10.

Density	1.05g/cm3
Boiling Point	437.2ºC at 760mmHg
Molecular Formula	C₂₄H₃₄N₄
Molecular Weight	378.55400
Flash Point	218.2ºC
Exact Mass	378.27800
PSA	33.95000
LogP	5.89730
Vapour Pressure	7.63E-08mmHg at 25°C
Index of Refraction	1.574

7H-Pyrrolo(2,3-d)pyrimidin-4-amine,N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)

Antalarmin

Antalarmin

Use of Antalarmin

Names

Antalarmin Biological Activity

Chemical & Physical Properties

Synonyms