AI Article Synopsis
- The text discusses a study on positive allosteric modulators (PAMs) that enhance the activity of muscarinic acetylcholine receptor 4 (M4).
- It highlights a specific compound, VU0467485, which is powerful and effective in models related to schizophrenia, showing promise for further development.
- The compound also has a favorable pharmacokinetic profile, making it a potential candidate for preclinical development.
Article Abstract
Herein, we report the structure-activity relationships within a series of potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M) positive allosteric modulators (PAMs). Compound (VU0467485) possesses robust M PAM potency across species and efficacy in preclinical models of schizophrenia. Coupled with an attractive DMPK profile and suitable predicted human PK, (VU0467485) was evaluated as a preclinical development candidate.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5304297 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.6b00461 | DOI Listing |
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