title: Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
abstract: Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo.
authors.affiliation: Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. dboatman@arenapharm.com
authors.forename: P Douglas
authors.initials: PD
authors.lastname: Boatman
authors.forename: Thomas O
authors.initials: TO
authors.lastname: Schrader
authors.forename: Michelle
authors.initials: M
authors.lastname: Kasem
authors.forename: Benjamin R
authors.initials: BR
authors.lastname: Johnson
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Skinner
authors.forename: Jae-Kyu
authors.initials: JK
authors.lastname: Jung
authors.forename: Jerry
authors.initials: J
authors.lastname: Xu
authors.forename: Martin C
authors.initials: MC
authors.lastname: Cherrier
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Webb
authors.forename: Graeme
authors.initials: G
authors.lastname: Semple
authors.forename: Carleton R
authors.initials: CR
authors.lastname: Sage
authors.forename: Jens
authors.initials: J
authors.lastname: Knudsen
authors.forename: Ruoping
authors.initials: R
authors.lastname: Chen
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Taggart
authors.forename: Ester
authors.initials: E
authors.lastname: Carballo-Jane
authors.forename: Jeremy G
authors.initials: JG
authors.lastname: Richman
mesh_terms: D000818:Animals; D004285:Dogs; D000882:Haplorhini; D006801:Humans; D051379:Mice; D011720:Pyrazoles / Q000737:chemistry*; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D011978:Receptors, Nicotinic / Q000378:metabolism; D013777:Tetrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: C530636:HCAR2 protein, human; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D013777:Tetrazoles; D014665:Vasodilator Agents; C031280:pyrazole