. 2014 Jul 10;9(9):1918–1928. doi: 10.1021/cb5004042

Table 1. Representative GPCRs Tagged with Fluorescent Ligands.

receptor	G protein	transduction mechanisms^b	physiological actions	fluorescent ligands
A_2A	G_s^a, G_olf, G_15,16^§	activates: AC^a, PLC	platelet aggregation inhibition;⁷¹ vasodilation;⁷² neurotransmitter release;⁷³ regulation of sensorimotor integration in basal ganglia;⁷⁴ sleep promotion⁷⁵	MRS5424, MRS5206, SCH442416^dy647
A_2A	G_s^a, G_olf, G_15,16^§	inhibits: Ca²⁺ channels		MRS5424, MRS5206, SCH442416^dy647
A₃	G_i/o^a	inhibits: AC^a	mast cell activation;⁷⁶preconditioning;⁷⁷ coronary vasodilation;⁷⁸ regulation of intraocular pressure;⁷⁹ hypotension⁸⁰	CA200645
A₃	G_i/o^a	activates: PLC		CA200645
D₂	G_i/o^a	inhibits: AC^a	modulation of locomotor activity;⁸¹ control of renal blood flow;⁸² learning and memory modulation⁸³	NAPS^dy647, NAPS^Lumio4Tb, spiperone^dy647
D₂	G_i/o^a	activates: GIRKs		NAPS^dy647, NAPS^Lumio4Tb, spiperone^dy647
μ, δ, κ	G_i/o^a, G_q/11, G_12/13	inhibits: AC	analgesia;⁸⁴ respiratory depression;⁸⁵ feeding;⁸⁶ neurotransmitter release;⁸⁷ body temperature regulation⁸⁸	naltrexone^dy647
μ, δ, κ	G_i/o^a, G_q/11, G_12/13	activates: PLC, GIRKs, PLA2, PLD		naltrexone^dy647
M₁	G_q/11^a	activates: PLC	bronchoconstriction;⁸⁹ vasodilation;⁹⁰ memory function;⁹¹ hypothermia;⁹² stimulation of water consumption⁹³ and urination⁹⁴	telenzepine^Cy3B, telenzepine^A488
ghrelin	G_q/11^a, G_i/o, G_12/13	activates: PLC	feeding⁹⁵ and release of GH⁹⁶	ghrelin^dy647
V_1A	G_q/11^a	activates: PLC	vasoconstriction;⁹⁷ hypertension;⁹⁸ platelet aggregation⁹⁹	[Lys⁸]PVA^A488, [Lys⁸]PVA^Eu⊂PBBP

Main mechanism of coupling.

AC, adenylyl cyclase; PLC, phospholipase C; PLA2, phospholipase A2; PLD, phospholipase D; GIRKs, G protein-dependent inwardly rectifying K+ channels.