title: GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
abstract: 5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan 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, USA. 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: Tom G
authors.initials: TG
authors.lastname: Holt
authors.forename: Michael S
authors.initials: MS
authors.lastname: Wolff
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 Gerard
authors.initials: MG
authors.lastname: 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; D005227:Fatty Acids / Q000378:metabolism; D006801:Humans; D051379:Mice; D009525:Niacin / Q000737:chemistry; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D011978:Receptors, Nicotinic / Q000378:metabolism
chemical_list: D005227:Fatty Acids; C530636:HCAR2 protein, human; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D009525:Niacin; C031280:pyrazole