a(MESH:"1-(3-(4-butyl-1-piperidinyl)propyl)-3,4-dihydro-2(1H)-quinolinone")
Subsequent optimization produced two analogs of AC-42 (AC-260584 and 77-LH-28-1), which maintained M1 selectivity and possessed properties suitable for use in animal models. Both AC-260584 and 77-LH-28-1 displayed antipsychotic and cognition-enhancing efficacy in pre-clinical models PubMed:24511233
Compound 77-LH-28-1 shows relatively higher selectivity for the M1 than for the M2, M4, and M5 subtypes, but retains weak agonist activity for M3 mAChR at high doses. Electrophysiological studies indicate that 77-LH-28-1 increases the activity of hippocampal CA1 pyramidal cells both in vitro and in vivo. Interestingly, unlike other normal orthosteric agonists, 77-LH-28-1 appears to selectively activate M1 mAChR in a distinct signaling pathway PubMed:24590577
Compound 77-LH-28-1 shows relatively higher selectivity for the M1 than for the M2, M4, and M5 subtypes, but retains weak agonist activity for M3 mAChR at high doses. Electrophysiological studies indicate that 77-LH-28-1 increases the activity of hippocampal CA1 pyramidal cells both in vitro and in vivo. Interestingly, unlike other normal orthosteric agonists, 77-LH-28-1 appears to selectively activate M1 mAChR in a distinct signaling pathway PubMed:24590577
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If you find BEL Commons useful in your work, please consider citing: Hoyt, C. T., Domingo-Fernández, D., & Hofmann-Apitius, M. (2018). BEL Commons: an environment for exploration and analysis of networks encoded in Biological Expression Language. Database, 2018(3), 1–11.