| Bioactivity | 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]. |
| Target | Ki: 2.7 nM (CRHR1) |
| Invitro | 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: |
| 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: |
| Name | Antalarmin |
| CAS | 157284-96-3 |
| Formula | C24H34N4 |
| Molar Mass | 378.55 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |