941573-59-7Relevant academic research and scientific papers
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, Corné,Wolfram, Dieter R.,Brussee, Johannes,Lane, J. Robert,Ijzerman, Adriaan P.
supporting information; experimental part, p. 3563 - 3567 (2012/06/04)
A number of pyrazolopyrimidines were synthesized and tested for their positive allosteric modulation of the HCA2 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.
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A
Shen, Hong C.,Taggart, Andrew K.P.,Wilsie, Larissa C.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
scheme or table, p. 4948 - 4951 (2009/05/07)
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
