Antalarmin

Names

[ CAS No. ]:
157284-96-3

[ Name ]:
Antalarmin

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

Biological Activity

[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.  

Chemical & Physical Properties

[ 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

Related Compounds