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. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445
Nomenclature HCA1 receptor HCA2 receptor HCA3 receptor
HGNC, UniProt HCAR1, Q9BXC0 HCAR2, Q8TDS4 HCAR3, P49019
Principal transduction Gi/o 1031,1034,1036. Gi/o 1040,1044,1045 Gi/o 1040,1045
Endogenous agonists (pKi) L-lactic acid (Selective) (pEC50 1.3 – 2.89) 1032,1034,1036,1041 β-D-hydroxybutyric acid (pEC50 3.1) 1042 3-hydroxyoctanoic acid (pEC50 5.1) 1031
Selective agonists (pKi) 3,5-dihydroxybenzoic acid (pEC50 3.72) 1035 MK 6892 (pEC50 7.8) 1039, MK 1903 (pEC50 7.56) 1033, nicotinic acid (pEC50 6.0 – 7.2) 1040,1044,1045, acipimox (pEC50 5.2 – 5.6) 1040,1045, monomethylfumarate (pEC50 5.03) 1043 1-isopropylbenzotriazole-5-carboxylic acid (pEC50 6.4) 1038
Radioligands (Kd) [3H]nicotinic acid (Agonist, Full agonist) (5.01x10-8 – 1x10-7 M) 1040,1044,1045