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. 2017 Oct 21;174(Suppl Suppl 1):S17–S129. doi: 10.1111/bph.13878
Nomenclature V 2 receptor OT receptor
HGNC, UniProt AVPR2, P30518 OXTR, P30559
Potency order of endogenous ligands vasopressin (AVP, P01185) >oxytocin (OXT, P01178) oxytocin (OXT, P01178) >vasopressin (AVP, P01185)
Endogenous agonists vasopressin (AVP, P01185) [24, 326, 334, 439, 1418, 1702, 1771, 1913, 1914, 1946, 2162] oxytocin (OXT, P01178) [24, 334, 335, 360, 682, 895]
Selective agonists VNA932 [527], OPC‐51803 [1418], d[Val 4,DArg8]VP [Thr 4,Gly7]OT [335, 500, 895]
Antagonists L‐371,257 (pK i 8.8) [682]
Selective antagonists conivaptan (pK i 9.4) [397], tolvaptan (pK i 9.4) [2162], satavaptan (pK i 8.4–9.3) [24, 383, 384, 1770, 1771, 1913, 1986], lixivaptan (Inverse agonist) (pK i 8.9–9.2) [33, 1771], d(CH 2)5[D‐Ile2,Ile4]AVP (pK i 6.9–8.4) [1771], mozavaptan (Inverse agonist) (pK i 7.4–8.1) [384, 1771, 1913, 1946, 2162, 2163] SSR126768A (pK i 8.8–9.1) [1772], desGlyNH 2‐d(CH2)5[Tyr(Me)2,Thr4,Orn8]OT (pK i 8.5), L‐372662 (pK i 8.4) [127]
Labelled ligands [3 H]AVP (human, mouse, rat) (Agonist) [334, 383, 384, 1418, 1702, 1913, 1914, 1946, 1986, 2162], [3 H]dDAVP (Agonist) [334, 384, 1946], [3 H]desGly‐NH 2[D‐Ile2,Ile4]VP (pK d 8.6) [125 I]d(CH 2)5[Tyr(Me)2,Thr4,Orn8,Tyr‐NH2 9]OVT (Antagonist) (pK d 10), [3 H]OT (human, mouse, rat) (Agonist) [334, 583, 895, 998], [111In]DOTA‐dLVT (pK d 8.3) [333]