Antalarmin

Modify Date: 2024-08-20 20:48:35

Antalarmin Structure
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].

 Names

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

 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
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

 Synonyms

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