| Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. | |
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MedLine Citation:
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PMID: 18752940 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Hong C Shen; Andrew K P Taggart; Larissa C Wilsie; M Gerard Waters; Milton L Hammond; James R Tata; Steven L Colletti |
Publication Detail:
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Type: Journal Article Date: 2008-08-14 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 18 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2008 Sep |
Date Detail:
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Created Date: 2008-09-15 Completed Date: 2008-10-14 Revised Date: 2011-11-03 |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 4948-51 Citation Subset: IM |
Affiliation:
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Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA. hong_shen@merck.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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