a(CHEBI:acetylcholine)
to p(HGNC:CHRM1)
Two novel M4-selective compounds, VU10010 and LY2033298, represented a breakthrough when they were described in 2008.84,85 VU10010 is a potent M4-selective PAM that increases affinity/efficacy of ACh to promote M4 mAChR activation.
act(a(CHEBI:acetylcholine)) increases act(p(HGNC:CHRM1))
c6fdb66235
The first subtype-selective M1 PAM to be characterized was benzyl quinolone carboxylic acid (BQCA);68 BQCA exhibited high selectivity with no activity at mAChR subtypes M2–M5 and induced up to a 129-fold leftward shift in ACh potency at the M1 mAChR
act(p(HGNC:CHRM1)) increases a(CHEBI:acetylcholine)
c14a9e658f
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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.