2. Academic Validation
  3. Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A

Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):4948-51. doi: 10.1016/j.bmcl.2008.08.039.
Hong C Shen 1,  Andrew K P Taggart,  Larissa C Wilsie,  M Gerard Waters,  Milton L Hammond,  James R Tata,  Steven L Colletti
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA. hong_shen@merck.com
PMID: 18752940 DOI: 10.1016/j.bmcl.2008.08.039
Abstract

Pyrazolopyrimidines were discovered as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. In addition to its intrinsic activity, compound 9n significantly enhances nicotinic acid binding to the receptor, thereby potentiating the functional efficacy of nicotinic acid.

Figures