Table 1.

Overview of biased ligands on selected GPCRs

Receptor	Biased ligand	Pathway	Therapeutic area	References
Angiotensin I receptor	SII	β-arrestin	Cardiovascular & Renal	Ahn et al., 2009; Boerrigter et al., 2011; Violin et al., 2010
	TRV120027
Apelin receptor	MM07	Gαi	Cardiovascular	Brame et al., 2015
Arginine-vasopressin	MCF14	Gαs	Renal	Jean-Alphonse et al., 2009
V2 receptor	MCF18
	MCF57
β1-adrenergic receptor	Carvedilol	β-arrestin	Cardiovascular	Kim et al., 2008, 2014
	Alprenolol
β2-adrenergic receptor	Fenoterol	Gαs	Pulmonary	Woo et al., 2009; Xiao et al., 2003
	Carvedilol	β-arrestin	Cardiovascular	Wisler et al., 2007
Dopamine D1 receptor	SKF83959	Gαq	Neurology & Behavior	Conroy et al., 2015; Rashid et al., 2007
	SKF38393
	SKF82957
	SKF75670
Dopamine D2 receptor	UNC9975	β-arrestin2	Neurology & Behavior	Chen et al., 2012; Park et al., 2016
	UNC9994
	MLS1547	Gαi/o	Neurology & Behavior	Free et al., 2014
Histamine H2 receptor	Famotidine	Gαs	Gastrointestinal	Alonso et al., 2015
Histamine H4 receptor	JNJ7777120	β-arrestin2	Inflammatory	Rosethorne and Charlton, 2011
κ-Opioid receptor (KOR)	Isoquinoline 2.1	Gαi/o	Neurology & Behavior	Zhou et al., 2013
	6′-GNTI			Rives et al., 2012
	RB-64			White et al., 2015
μ-Opioid receptor (MOR)	TRV130	Gαi/o	Neurology & Behavior	Chen et al., 2013; DeWire et al., 2013
	NAP	Gαi/o	Neurology & Behavior	Zhang et al., 2016
Serotonin 5-HT2B receptor	Ergotamin	β-arrestin	Neurology & Behavior	Wacker et al., 2013