AI Article Synopsis
- - A new positive allosteric modulator (PAM), (S)-9b, was discovered through a high throughput screening process aimed at enhancing glucagon-like peptide-1 receptor (GLP-1R) activity.
- - (S)-9b increased the effectiveness of low-dose exenatide, leading to improved insulin secretion in mouse pancreatic islets.
- - The compound also showed potential in reversing catalepsy caused by haloperidol by boosting the activity of endogenous GLP-1R.
Article Abstract
A duplexed, functional multiaddition high throughput screen and subsequent iterative parallel synthesis effort identified the first highly selective and CNS penetrant glucagon-like peptide-1R (GLP-1R) positive allosteric modulator (PAM). PAM (S)-9b potentiated low-dose exenatide to augment insulin secretion in primary mouse pancreatic islets, and (S)-9b alone was effective in potentiating endogenous GLP-1R to reverse haloperidol-induced catalepsy.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4266362 | PMC |
| http://dx.doi.org/10.1021/jm501375c | DOI Listing |
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