AI Article Synopsis
- - A series of pyrimidine analogues from ATC0175 were developed and found to effectively block the human MCH-R1 receptor in lab tests.
- - Some analogues showed better selectivity for the receptor, but there was no enhancement in how well they could penetrate the brain.
- - One analogue could reduce food intake and body weight in a long-term study, but researchers couldn't link this effect to its concentration in the brain, suggesting it might not work through the MCH-R1 receptor.
Article Abstract
A series of pyrimidine analogues derived from ATC0175 were potent antagonists of human MCH-R1 in vitro. Significantly improved receptor selectivity was achieved with several analogues from this series, but no improvement in brain partitioning was noted. One example from this series was shown to inhibit food intake and decrease body weight in a chronic study. However no clear correlation between the pharmacodynamic effect and the pharmacokinetic data with respect to brain concentration was discernible leading us to conclude that the observed effect was most likely not due to interaction with the MCH-R1.
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| http://dx.doi.org/10.1016/j.bmcl.2009.09.003 | DOI Listing |
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