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] |