Vasopressin and oxytocin receptors
More information on this family may be found on the IUPHAR-DB family and introduction pages.
Vasopressin (AVP) and oxytocin (OT) receptors (nomenclature as agreed by NC-IUPHAR Subcommittee on vasopressin and oxytoxcin receptors) are activated by the endogenous cyclic nonapeptides AVP and oxytocin (OT). These peptides are derived from precursors (ENSG00000101200 and ENSG00000101405 respectively), which also produce neurophysins.
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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13. Cotte, N., Balestre, M. N., Phalipou, S., Hibert, M., Manning, M., Barberis, C. and Mouillac, B. (1998) Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor. J Biol Chem, 273: 29462-29468. [PMID:9792651]
14. Derick, S., Cheng, L. L., Stoev, S., Voirol, M. J., Ben Mimoun, M., Andres, M., Gaillard, R., Guillon, G. and Manning, M. (2002) [1-Deamino-4-Cyclohexylalanine]Arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology., 143: 4655-4664. [PMID:12446593]
15. Elands, J; Barberis, C; Jard, S. (1988) [3H]-[Thr4,Gly7]OT: a highly selective ligand for central and peripheral OT receptors. Am. J. Physiol., 254 (1 Pt 1): E31-8. [PMID:2827511]
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19. Griffante, C., Green, A., Curcuruto, O., Haslam, C. P., Dickinson, B. A. and Arban, R. (2005) Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. Br J Pharmacol, 146: 744-751. [PMID:16158071]
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30. Serradeil-Le Gal, C., Valette, G., Foulon, L., Germain, G., Advenier, C., Naline, E., Bardou, M., Martinolle, J-P., Pouzet, B., Raufaste, D., Garcia, C., Double-Cazenave, E., Pauly, M., Pascal, M., Barbier, A., Scatton, B., Maffrand, J-P. and Le Fur, G. (2004) SSR126768A (4-Chloro-3-[(3R)-(+)-5-chloro-1-(2,4-dimethoxybenzyl)-3-methyl-2oxo-2,3-dihydro-1H-indol-3-yl]-N-ethyl-N-(3-pyridylmethyl)-benzamidine, hydrochloride): a new selective and orally active oxytocin receptor antagonist for the prevention of preterm labor. J Pharmacol Exp Therap, 309: 414-424. [PMID:14722330]
31. Serradeil-Le Gal, C., Wagnon, J., Simiand, J., Griebel, G., Lacour, C., Guillon, G., Barberis, C., Brossard, G., Soubrie, P., Nisato, D., Pascal, M., Pruss, R., Scatton, B., Maffrand, J. P. and Le Fur, G. (2002) Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist. J Pharmacol Exp Ther, 300: 1122-1130. [PMID:11861823]
32. Tahara, A., Saito, M., Sugimoto, J., Tomura, Y., Wada, K. I., Kusayama, T., Tsukada, J., Ishii, I., Yatsu, T., Uchida, W. and Tanaka, A. (1998) Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in chinese hamster ovary cells. Br J Pharmacol, 125: 1463-1470. [PMID:9884074]
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37. Yamamura, Y., Nakamura, S., Itoh, S., Hirano, T., Onogawa, T., Yamashita, T., Yamada, Y., Tsujimae, K., Aoyama, M., Kotosai, K., Ogawa, H., Yamashita, H., Kondo, K., Tominaga, M., Tsujimoto, G. and Mori, T. (1998) OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats. J Pharmacol Exp Ther, 287: 860-867. [PMID:9864265]
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The V2 receptor exhibits marked species differences, such that many ligands (d(CH2)5[D-Ile2,Ile4]AVP and [3H]desGly-NH2[D-Ile2,Ile4]VP) exhibit low affinity at human V2 receptors [2]. Similarly, [3H]d[D-Arg8]VP is V2 selective in the rat, not in the human [27]. The gene encoding the V2 receptor is polymorphic in man, underlying nephrogenic diabetes insipidus [6]. conivaptan display high affinity for both human V1a and V2 receptors [33]. d[Cha4]AVP is selective only for the human and bovine V1b receptors [14], while d[Leu4]LVP has high affinity for the rat V1b receptor [24].