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Bioorg Med Chem Lett. 2007 May 15;17(10):2869-73. Epub 2007 Feb 25.

PDE-10A inhibitors as insulin secretagogues.

Author information

1
Department of Chemistry Research, Bayer Pharmaceuticals Corporation, West Haven, CT 06516, USA. Louis-David.Cantin.Cantin@astrazeneca.com

Abstract

Modulation of cAMP levels has been linked to insulin secretion in preclinical animal models and in humans. The high expression of PDE-10A in pancreatic islets suggested that inhibition of this enzyme may provide the necessary modulation to elicit increased insulin secretion. Using an HTS approach, we have identified quinoline-based PDE-10A inhibitors as insulin secretagogues in vitro. Optimized compounds were evaluated in vivo where improvements in glucose tolerance and increases in insulin secretion were measured.

PMID:
17400452
DOI:
10.1016/j.bmcl.2007.02.061
[Indexed for MEDLINE]

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