Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia
2017
Herein, we report the
structure–activity relationshipswithin a series of potent, selective, and orally bioavailable
muscarinic acetylcholine receptor4 (M4) positive
allosteric modulators(PAMs). Compound 6c (VU0467485) possesses robust in vitro M4 PAM potency across species and in vivo efficacy in preclinical models of schizophrenia. Coupled with an attractive DMPK profile and suitable predicted human PK, 6c (VU0467485) was evaluated as a preclinical development candidate.
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