BQCA (benzylquinolone carboxylic acid) a highly selective allosteric M1 mAChR modulator.

BQCA提高了M1受体对乙酰胆碱的亲和力。BQCA激活M1受体在(mPFC)锥体细胞中引发强烈的内向电流，增加自发性兴奋性突触后电流。

BQCA通过促进β-arrestin招募至M1，表明该信号转导机制在乙酰胆碱调节记忆中的作用。BQCA能逆转东莨菪碱引起的在情境恐惧条件下的记忆缺陷，增加大脑皮层的血流量，并增加清醒状态同时减少深度睡眠。BQCA在体内增加mPFC锥体细胞的放电。BQCA同样在阿尔茨海默病的转基因小鼠模型中恢复辨别反转学习。

Competition binding reactions used 25 μg human M1 CHO membrane protein, BQCA or vehicle, and 0.15 nM [3H]NMS in 96-well deep-well plates. Binding reactions (30 °C for 2-3 h) are terminated by rapid filtration. Nonspecific binding is determined by adding 10 μM atropine. Filter plates are ished 4×with ice-cold 20 mM HEPES, 100 mM NaCl, and 5 mM MgCl2, pH 7.4 using a 96-well harvester. Plates are dried and radioactivity counted with a microplate scintillation counter[1].