Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 8, Issue 2, Pages 233-238Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00461
Keywords
Positive allosteric modulator (PAM); muscarinic acetylcholine receptor 4 (M-4); VU0467485; schizophrenia
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Funding
- William K. Warren Foundation
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Herein, we report the structure-activity relationships within a series of potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M-4) positive allosteric modulators (PAMs). Compound 6c (VU0467485) possesses robust in vitro M-4 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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