title: GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.
abstract: 5-Alkyl and aryl-pyrazole-tetrazoles have been identified as a new class of selective, small-molecule, agonists of the human G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, Inc, Rahway, NJ 07065-0900, United States. jason_imbriglio@merck.com
authors.forename: Jason E
authors.initials: JE
authors.lastname: Imbriglio
authors.forename: Sookhee
authors.initials: S
authors.lastname: Chang
authors.forename: Rui
authors.initials: R
authors.lastname: Liang
authors.forename: Subharekha
authors.initials: S
authors.lastname: Raghavan
authors.forename: Darby
authors.initials: D
authors.lastname: Schmidt
authors.forename: Abby
authors.initials: A
authors.lastname: Smenton
authors.forename: Scott
authors.initials: S
authors.lastname: Tria
authors.forename: Thomas O
authors.initials: TO
authors.lastname: Schrader
authors.forename: Jae-Kyu
authors.initials: JK
authors.lastname: Jung
authors.forename: Craig
authors.initials: C
authors.lastname: Esser
authors.forename: Andrew K P
authors.initials: AK
authors.lastname: Taggart
authors.forename: Kang
authors.initials: K
authors.lastname: Cheng
authors.forename: Ester
authors.initials: E
authors.lastname: Carballo-Jane
authors.forename: M
authors.initials: M
authors.lastname: Gerard Waters
authors.forename: James R
authors.initials: JR
authors.lastname: Tata
authors.forename: Steven L
authors.initials: SL
authors.lastname: Colletti
mesh_terms: D000818:Animals; D006801:Humans; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D018345:Mice, Knockout; D018722:Nicotinic Agonists / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000172:deficiency / Q000502:physiology; D011978:Receptors, Nicotinic / Q000172:deficiency / Q000502:physiology; D013777:Tetrazoles / Q000737:chemistry* / Q000494:pharmacology; D014664:Vasodilation / Q000187:drug effects / Q000502:physiology
chemical_list: C530636:HCAR2 protein, human; D018722:Nicotinic Agonists; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D013777:Tetrazoles; C031280:pyrazole