Document Detail


Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
MedLine Citation:
PMID:  18752940     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Hong C Shen; Andrew K P Taggart; Larissa C Wilsie; M Gerard Waters; Milton L Hammond; James R Tata; Steven L Colletti
Publication Detail:
Type:  Journal Article     Date:  2008-08-14
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  18     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2008 Sep 
Date Detail:
Created Date:  2008-09-15     Completed Date:  2008-10-14     Revised Date:  2011-11-03    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  4948-51     Citation Subset:  IM    
Affiliation:
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA. hong_shen@merck.com
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MeSH Terms
Descriptor/Qualifier:
Binding Sites
Combinatorial Chemistry Techniques
Humans
Molecular Structure
Niacin / metabolism
Nicotinic Agonists / chemical synthesis*,  chemistry,  pharmacology*
Pyrazoles / chemical synthesis*,  chemistry,  pharmacology*
Pyrimidines / chemical synthesis*,  chemistry,  pharmacology*
Receptors, G-Protein-Coupled / agonists*
Receptors, Nicotinic
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/HCAR2 protein, human; 0/HCAR3 protein, human; 0/Nicotinic Agonists; 0/Pyrazoles; 0/Pyrimidines; 0/Receptors, G-Protein-Coupled; 0/Receptors, Nicotinic; 59-67-6/Niacin

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