GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.
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.
Imbriglio
Jason E
JE
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, Inc, Rahway, NJ 07065-0900, United States. jason_imbriglio@merck.com
Chang
Sookhee
S
Liang
Rui
R
Raghavan
Subharekha
S
Schmidt
Darby
D
Smenton
Abby
A
Tria
Scott
S
Schrader
Thomas O
TO
Jung
Jae-Kyu
JK
Esser
Craig
C
Taggart
Andrew K P
AK
Cheng
Kang
K
Carballo-Jane
Ester
E
Gerard Waters
M
M
Tata
James R
JR
Colletti
Steven L
SL
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
C530636:HCAR2 protein, human; D018722:Nicotinic Agonists; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D013777:Tetrazoles; C031280:pyrazole