TBPB is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; EC50 = 158 nM in CHO-K1 cells expressing rat recombinant receptors).1 It is selective for M1 over M2-5 receptors at concentrations up to 10 μM. TBPB (3 μM) potentiates NMDA-evoked currents in CA1 pyramidal cells. It increases production of the non-amyloidogenic amyloid precursor protein (APP) cleavage products APPsα and CTFα in PC12 cells overexpressing the human M1 receptor and APP when used at a concentration of 1 μM. TBPB decreases amphetamine-induced hyperlocomotion in a rat model that is predictive of antipsychotic-like activity.
1.Jones, C.K., Brady, A.E., Davis, A.A., et al.Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in ratsJ. Neurosci.28(41)10422-10433(2008)