AC 187 TFA 是一种有效且具有口服活性的胰淀素受体 (amylin receptor) 拮抗剂，IC50 为 0.48 nM，Ki 为 0.275 nM。AC 187 TFA 对胰淀素受体的选择性高于降钙素和 CGRP 受体。AC 187 TFA 具有神经保护作用。
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects[1][2].
AC 187 blocks amyloidβ protein (Aβ)-induced neurotoxicity. Treatment of cultures with AC 187 before exposure to Aβ results in significantly improved neuronal survival[1].AC187 attenuates the activation of initiator and effector caspases that mediate Aβ-induced apoptotic cell death[1].
AC 187 (30 mg/mL) increases glucagon concentration, accelerates gastric emptying of liquids, and results in an exaggerated post-challenge glycemia in hyperinsulinemic clamps in Sprague-Dawley (HSD) rats[2].
[1]. Jack H Jhamandas, et al. Antagonist of the amylin receptor blocks beta-amyloid toxicity in rat cholinergic basal forebrain neurons. J Neurosci. 2004 Jun 16;24(24):5579-84.
[2]. Bronislava R Gedulin, et al. Role of endogenous amylin in glucagon secretion and gastric emptying in rats demonstrated with the selective antagonist, AC187. Regul Pept. 2006 Dec 10;137(3):121-7.
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