The Concise Guide to PHARMACOLOGY 2015/16: G protein‐coupled receptors

. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348

Nomenclature	MT₁ receptor	MT₂ receptor
HGNC, UniProt	MTNR1A, P48039	MTNR1B, P49286
Endogenous agonists	melatonin (pK _i 9.1–9.7) [67, 445, 447]	melatonin (pK _i 9.4–9.8) [67, 445, 447]
Agonists	ramelteon (pK _i 10.9) [909], agomelatine (pK _i 10–10.4) [67, 132]	agomelatine (pK _i 9.9–10.5) [67, 132], ramelteon (pK _i 10) [909, 1565]
Selective agonists	–	IIK7 (pK _i 10.3) [506, 1814], 5‐methoxy‐luzindole (Partial agonist) (pK _i 9.6) [447]
Selective antagonists	–	4P‐PDOT (pK _i 8.8–9.4) [67, 447, 448], K185 (pK _i 9.3) [506, 1814], DH97 (pK _i 8) [1865]
Labelled ligands	[¹²⁵I]SD6 (Agonist) (pK _d 10.9) [1074], 2‐[¹²⁵I]melatonin (Agonist) (pK _d 9.9–10.7) [67, 447], [³H]melatonin (Agonist) (pK _d 9.4–9.9) [230]	[¹²⁵I]SD6 (Agonist) (pK _d 10.2) [1074], 2‐[¹²⁵I]melatonin (Agonist) (pK _d 9.7–10) [67, 447], [¹²⁵I]DIV880 (Agonist, Partial agonist) (pK _d 9.7) [1074], [³H]melatonin (Agonist) (pK _d 9–9.6) [230]