Skip to main content

Research Repository

Advanced Search

Novel 3, 6, 7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A)

Blad, Clara C; van Veldhoven, Jacobus P D; Klopman, Corn�; Wolfram, Dieter R; Brussee, Johannes; Lane, J Robert; Ijzerman, Adriaan P

Authors

Clara C Blad

Jacobus P D van Veldhoven

Corn� Klopman

Dieter R Wolfram

Johannes Brussee

J Robert Lane

Adriaan P Ijzerman



Abstract

A number of pyrazolopyrimidines were synthesized and tested for their positive allosteric modulation of the HCA(2) receptor (GPR109A). Compound 24, an efficacious and potent agonist and allosteric enhancer of nicotinic acid's action, was the basis for most other compounds. Interestingly, some of the compounds were found to increase the efficacy of the endogenous ligand 3-hydroxybutyrate and enhance its potency almost 10-fold. This suggests that the pyrazolopyrimidines may have therapeutic value when given alone.

Citation

Blad, C. C., van Veldhoven, J. P. D., Klopman, C., Wolfram, D. R., Brussee, J., Lane, J. R., & Ijzerman, A. P. (2012). Novel 3, 6, 7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A). Journal of Medicinal Chemistry, 55(7), 3563-3567. https://doi.org/10.1021/jm300164q

Journal Article Type Article
Acceptance Date Oct 24, 2011
Online Publication Date Mar 27, 2012
Publication Date Mar 15, 2012
Deposit Date Apr 22, 2020
Journal Journal of Medicinal Chemistry
Print ISSN 0022-2623
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 55
Issue 7
Pages 3563-3567
DOI https://doi.org/10.1021/jm300164q
Public URL http://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=22420767&retmode=ref&cmd=prlinks
Publisher URL https://pubs.acs.org/doi/full/10.1021/jm300164q

Downloadable Citations