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Molecular Pharmacology of Human Vasopressin Receptors

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Vasopressin and Oxytocin

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 449))

Abstract

Vasopressin (AVP) and oxytocin (OT) are cyclic nonapeptides whose actions are mediated by activation of specific G protein-coupled receptors (GPCRs) currently classified into V1-vascular (V1R), V2-renal (V2R) and V3-pituitary (V3R) AVP receptors and OT receptors (OTR). The cloning of the different members of the AVP/OT family of receptors now allows the extensive molecular pharmacological characterization of a single AVP/OT receptor subtype in stably transfected mammalian cell lines.

The human V1-vascular (CHO-V1), V2-renal (CHO-V2), V3-pituitary (CHO-V3) and oxytocin (CHO-OT) receptors stably expressed in CHO cells display distinct binding profiles for 18 peptide and 5 nonpeptide AVP/OT analogs. Several peptide and nonpeptide compounds have a greater affinity for the V1R than AVP itself. V2R peptide agonists and antagonists tend to be non-selective ligands whereas nonpeptide V2R antagonists are potent and subtype-selective. None of the 22 AVP/OT analogs tested has a better affinity for the human V3R than AVP itself. Several peptide antagonists do not select well between V1R and OTR. These results underscore the need for developing specific and potent analogs interacting specifically with a given human AVP/OT receptor subtype.

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Authors and Affiliations

  1. Departments of Medicine and Physiology, Case Western Reserve University School of Medicine, 10900 Euclid Avenue, Cleveland, Ohio, 44106-4951, USA

    Rafael Mattera

  2. Division of Clinical and Molecular Endocrinology, Department of Medicine, Case Western Reserve University School of Medicine, 10900 Euclid Avenue, Room BRB431, Cleveland, Ohio, 44106-4951, USA

    Dr. Marc Thibonnier

Authors
  1. Dr. Marc Thibonnier
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  2. Doreen M. Conarty
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  3. Judith A. Preston
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  4. Pamela L. Wilkins
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  5. Liliana N. Berti-Mattera
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  6. Rafael Mattera
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Correspondence to Marc Thibonnier .

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Editors and Affiliations

  1. McGill University, Montreal, Quebec, Canada

    Hans H. Zingg  & Charles W. Bourque  & 

  2. University of Montreal, Montreal, Quebec, Canada

    Daniel G. Bichet

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Thibonnier, M., Conarty, D.M., Preston, J.A., Wilkins, P.L., Berti-Mattera, L.N., Mattera, R. (1998). Molecular Pharmacology of Human Vasopressin Receptors. In: Zingg, H.H., Bourque, C.W., Bichet, D.G. (eds) Vasopressin and Oxytocin. Advances in Experimental Medicine and Biology, vol 449. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-4871-3_34

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  • DOI: https://doi.org/10.1007/978-1-4615-4871-3_34

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