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Gene Review

AVPR1A  -  arginine vasopressin receptor 1A

Homo sapiens

Synonyms: AVPR V1a, AVPR1, Antidiuretic hormone receptor 1a, V1aR, Vascular/hepatic-type arginine vasopressin receptor, ...
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Disease relevance of AVPR1A


Psychiatry related information on AVPR1A


High impact information on AVPR1A

  • The neurohypophysial hormone arginine vasopressin (AVP) is a cyclic nonpeptide whose actions are mediated by the stimulation of specific G protein--coupled membrane receptors pharmacologically classified into V1-vascular (V1R), V2-renal (V2R) and V3-pituitary (V3R) AVP receptor subtypes [11].
  • In parallel, the abundance of vasopressin V1a receptors and the proportion of V1a receptor-labeled dendritic spines increase [12].
  • Moreover, when Tyr115 is replaced by an Asp and a Phe, the amino acids naturally occurring in the V2 and in the OT receptor subtypes, the agonist selectivity of the V1a receptor switches accordingly [13].
  • In this study, we investigated the functional roles of the V1a receptor in cardiovascular homeostasis using gene targeting [14].
  • Taken together, these results indicate that the V1a receptor plays an important role in normal resting arterial BP regulation mainly by its regulation of circulating blood volume and baroreflex sensitivity [14].

Chemical compound and disease context of AVPR1A


Biological context of AVPR1A


Anatomical context of AVPR1A


Associations of AVPR1A with chemical compounds


Physical interactions of AVPR1A

  • Our data establish that a single residue, Arg46, is critical for AVP binding to the V1aR [29].
  • Requirement of the third intracellular loop of the V2R for G(s) activation was identified by introducing V2R segments into the Gq coupled V1aR [Liu, J. and Wess, J. (1996) J. Biol. Chem. 271, 8772-8778]; the same approach recognized glutamate 231 and glutamine 225 at the amino terminus of loop 3i as being needed for signal transduction [30].

Regulatory relationships of AVPR1A


Other interactions of AVPR1A

  • Within the family of human AVP receptors, the V2 AVP receptor has been cloned, but the structure of the human V1a and V1b AVP receptors remains unknown [34].
  • Similar docking modes were found for the YM087/V1aR and YM087/V2R complexes, diverse from those of the YM087/OTR complexes, in agreement with the molecular affinity data [35].
  • YM087 was computer-docked to V1aR, V2R and OTR using the AutoDock (Olson et al., Scripps Research Institute, La Jolla, USA) and subsequently relaxed using restrained simulated annealing and molecular dynamics, as implemented in AMBER program (Kollman et al., University of California, San Francisco, USA) [35].
  • The V1a vasopressin receptor (V1aR) is a member of the neurohypophysial hormone subfamily of G protein-coupled receptors [28].
  • In vivo and in vitro effects of AVP and V1a receptor antagonist on Cushing's syndrome due to ACTH-independent bilateral macronodular adrenocortical hyperplasia [15].

Analytical, diagnostic and therapeutic context of AVPR1A


  1. Study of V(1)-vascular vasopressin receptor gene microsatellite polymorphisms in human essential hypertension. Thibonnier, M., Graves, M.K., Wagner, M.S., Chatelain, N., Soubrier, F., Corvol, P., Willard, H.F., Jeunemaitre, X. J. Mol. Cell. Cardiol. (2000) [Pubmed]
  2. Pathophysiology of renal fluid retention. Schrier, R.W., Fassett, R.G., Ohara, M., Martin, P.Y. Kidney Int. Suppl. (1998) [Pubmed]
  3. Increased water intake decreases progression of polycystic kidney disease in the PCK rat. Nagao, S., Nishii, K., Katsuyama, M., Kurahashi, H., Marunouchi, T., Takahashi, H., Wallace, D.P. J. Am. Soc. Nephrol. (2006) [Pubmed]
  4. Eutopic overexpression of vasopressin v1a receptor in adrenocorticotropin-independent macronodular adrenal hyperplasia. Mune, T., Murase, H., Yamakita, N., Fukuda, T., Murayama, M., Miura, A., Suwa, T., Hanafusa, J., Daido, H., Morita, H., Yasuda, K. J. Clin. Endocrinol. Metab. (2002) [Pubmed]
  5. Development and therapeutic indications of orally-active non-peptide vasopressin receptor antagonists. Paranjape, S.B., Thibonnier, M. Expert opinion on investigational drugs. (2001) [Pubmed]
  6. Transmission disequilibrium testing of arginine vasopressin receptor 1A (AVPR1A) polymorphisms in autism. Kim, S.J., Young, L.J., Gonen, D., Veenstra-VanderWeele, J., Courchesne, R., Courchesne, E., Lord, C., Leventhal, B.L., Cook, E.H., Insel, T.R. Mol. Psychiatry (2002) [Pubmed]
  7. Association between a vasopressin receptor AVPR1A promoter region microsatellite and eating behavior measured by a self-report questionnaire (Eating Attitudes Test) in a family-based study of a nonclinical population. Bachner-Melman, R., Zohar, A.H., Elizur, Y., Nemanov, L., Gritsenko, I., Konis, D., Ebstein, R.P. The International journal of eating disorders. (2004) [Pubmed]
  8. Are the arginine vasopressin V1a receptor microsatellites related to hypersexuality in children with a prepubertal and early adolescent bipolar disorder phenotype? Geller, B., Tillman, R., Badner, J.A., Cook, E.H. Bipolar disorders. (2005) [Pubmed]
  9. A major SNP haplotype of the arginine vasopressin 1B receptor protects against recurrent major depression. van West, D., Del-Favero, J., Aulchenko, Y., Oswald, P., Souery, D., Forsgren, T., Sluijs, S., Bel-Kacem, S., Adolfsson, R., Mendlewicz, J., Van Duijn, C., Deboutte, D., Van Broeckhoven, C., Claes, S. Mol. Psychiatry (2004) [Pubmed]
  10. Effect of arginine vasopressin in the nucleus raphe magnus on antinociception in the rat. Yang, J., Chen, J.M., Liu, W.Y., Song, C.Y., Wang, C.H., Lin, B.C. Peptides (2006) [Pubmed]
  11. The basic and clinical pharmacology of nonpeptide vasopressin receptor antagonists. Thibonnier, M., Coles, P., Thibonnier, A., Shoham, M. Annu. Rev. Pharmacol. Toxicol. (2001) [Pubmed]
  12. Fatherhood affects dendritic spines and vasopressin V1a receptors in the primate prefrontal cortex. Kozorovitskiy, Y., Hughes, M., Lee, K., Gould, E. Nat. Neurosci. (2006) [Pubmed]
  13. Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. Chini, B., Mouillac, B., Ala, Y., Balestre, M.N., Trumpp-Kallmeyer, S., Hoflack, J., Elands, J., Hibert, M., Manning, M., Jard, S. EMBO J. (1995) [Pubmed]
  14. V1a vasopressin receptors maintain normal blood pressure by regulating circulating blood volume and baroreflex sensitivity. Koshimizu, T.A., Nasa, Y., Tanoue, A., Oikawa, R., Kawahara, Y., Kiyono, Y., Adachi, T., Tanaka, T., Kuwaki, T., Mori, T., Takeo, S., Okamura, H., Tsujimoto, G. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  15. In vivo and in vitro effects of AVP and V1a receptor antagonist on Cushing's syndrome due to ACTH-independent bilateral macronodular adrenocortical hyperplasia. Daidoh, H., Morita, H., Hanafusa, J., Mune, T., Murase, H., Sato, M., Shibata, T., Suwa, T., Ishizuka, T., Yasuda, K. Clin. Endocrinol. (Oxf) (1998) [Pubmed]
  16. New agents for managing hyponatremia in hospitalized patients. Munger, M.A. American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists (2007) [Pubmed]
  17. Involvement of oxytocin and vasopressin in the pathophysiology of preterm labor and primary dysmenorrhea. Akerlund, M. Prog. Brain Res. (2002) [Pubmed]
  18. The effect of relcovaptan (SR 49059), an orally active vasopressin V1a receptor antagonist, on uterine contractions in preterm labor. Steinwall, M., Bossmar, T., Brouard, R., Laudanski, T., Olofsson, P., Urban, R., Wolff, K., Le-Fur, G., Akerlund, M. Gynecol. Endocrinol. (2005) [Pubmed]
  19. Oxytocin, vasopressin and pair bonding: implications for autism. Hammock, E.A., Young, L.J. Philos. Trans. R. Soc. Lond., B, Biol. Sci. (2006) [Pubmed]
  20. Structure, sequence, expression, and chromosomal localization of the human V1a vasopressin receptor gene. Thibonnier, M., Graves, M.K., Wagner, M.S., Auzan, C., Clauser, E., Willard, H.F. Genomics (1996) [Pubmed]
  21. Molecular pharmacology and modeling of vasopressin receptors. Thibonnier, M., Coles, P., Thibonnier, A., Shoham, M. Prog. Brain Res. (2002) [Pubmed]
  22. Oxytocin receptors expressed and coupled to Ca2+ signalling in a human vascular smooth muscle cell line. Yazawa, H., Hirasawa, A., Horie, K., Saita, Y., Iida, E., Honda, K., Tsujimoto, G. Br. J. Pharmacol. (1996) [Pubmed]
  23. Human vascular vasopressin receptors: analysis with selective vasopressin receptor antagonists. Ohlstein, E.H., Berkowitz, B.A. J. Pharmacol. Exp. Ther. (1986) [Pubmed]
  24. Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women. Akerlund, M., Bossmar, T., Brouard, R., Kostrzewska, A., Laudanski, T., Lemancewicz, A., Serradeil-Le Gal, C., Steinwall, M. British journal of obstetrics and gynaecology. (1999) [Pubmed]
  25. Novel approach to the design of synthetic radioiodinated linear V1A receptor antagonists of vasopressin. Manning, M., Bankowski, K., Barberis, C., Jard, S., Elands, J., Chan, W.Y. Int. J. Pept. Protein Res. (1992) [Pubmed]
  26. Desensitization of the human V2 vasopressin receptor. Homologous effects in the absence of heterologous desensitization. Birnbaumer, M., Antaramian, A., Themmen, A.P., Gilbert, S. J. Biol. Chem. (1992) [Pubmed]
  27. Examination of AVPR1a as an autism susceptibility gene. Wassink, T.H., Piven, J., Vieland, V.J., Pietila, J., Goedken, R.J., Folstein, S.E., Sheffield, V.C. Mol. Psychiatry (2004) [Pubmed]
  28. The N-terminal juxtamembrane segment of the V1a vasopressin receptor provides two independent epitopes required for high-affinity agonist binding and signaling. Hawtin, S.R., Wesley, V.J., Simms, J., Argent, C.C., Latif, K., Wheatley, M. Mol. Endocrinol. (2005) [Pubmed]
  29. A single residue (arg46) located within the N-terminus of the V1a vasopressin receptor is critical for binding vasopressin but not peptide or nonpeptide antagonists. Hawtin, S.R., Wesley, V.J., Parslow, R.A., Simms, J., Miles, A., McEwan, K., Wheatley, M. Mol. Endocrinol. (2002) [Pubmed]
  30. A role for K268 in V2R folding. Gouill, C.L., Darden, T., Madziva, M.T., Birnbaumer, M. FEBS Lett. (2005) [Pubmed]
  31. Physiological effects of vasopressin and atrial natriuretic peptide in the collecting duct. Inoue, T., Nonoguchi, H., Tomita, K. Cardiovasc. Res. (2001) [Pubmed]
  32. Heterodimerization of V1a and V2 vasopressin receptors determines the interaction with beta-arrestin and their trafficking patterns. Terrillon, S., Barberis, C., Bouvier, M. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  33. Role of septal vasopressin innervation in paternal behavior in prairie voles (Microtus ochrogaster). Wang, Z., Ferris, C.F., De Vries, G.J. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  34. Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor. Thibonnier, M., Auzan, C., Madhun, Z., Wilkins, P., Berti-Mattera, L., Clauser, E. J. Biol. Chem. (1994) [Pubmed]
  35. Molecular modeling of interactions of the non-peptide antagonist YM087 with the human vasopressin V1a, V2 receptors and with oxytocin receptors. Giełdoń, A., Kaźmierkiewicz, R., Slusarz, R., Ciarkowski, J. J. Comput. Aided Mol. Des. (2001) [Pubmed]
  36. Vasopressin receptors in human adrenal medulla and pheochromocytoma. Grazzini, E., Breton, C., Derick, S., Andres, M., Raufaste, D., Rickwaert, F., Boccara, G., Colson, P., Guérineau, N.C., Serradeil-le Gal, C., Guillon, G. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  37. Expression of the Oxytocin and V1a Vasopressin Receptors in Human Myometrium in Differing Physiologic States and following Misoprostol Administration. Wing, D.A., Goharkhay, N., Felix, J.C., Rostamkhani, M., Naidu, Y.M., Kovacs, B.W. Gynecol. Obstet. Invest. (2006) [Pubmed]
  38. Neurological impact of vasopressin dysregulation and hyponatremia. Bhardwaj, A. Ann. Neurol. (2006) [Pubmed]
  39. Vasopressin and serotonin interactions in the control of agonistic behavior. Ferris, C.F., Delville, Y. Psychoneuroendocrinology (1994) [Pubmed]
  40. Overview of vasopressin receptor antagonists in heart failure resulting in hospitalization. De Luca, L., Orlandi, C., Udelson, J.E., Fedele, F., Gheorghiade, M. Am. J. Cardiol. (2005) [Pubmed]
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