"目录号: HY-14562
GPCR/G ProteinNeuronal Signaling-
TBPB是M1 mAChR变构激动剂，EC50值为289nM，调节amyloid的加工和小鼠体内具有抗精神病药物等活性。
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生物活性
Description
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.IC50 value: 289 nM(EC50) [2]Target: M1 mAChR agonistin vitro: TBPB activates M(1) through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its unprecedented selectivity. Whole-cell patch-clamp recordings demonstrated that activation of M(1) by TBPB potentiates NMDA receptor currents in hippocampal pyramidal cells but does not alter excitatory or inhibitory synaptic transmission, responses thought to be mediated by M(2) and M(4) [1]. in vivo: TBPB was efficacious in models predictive of antipsychotic-like activity in rats at doses that did not produce catalepsy or peripheral adverse effects of other mAChR agonists [1].
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