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Analogues of arginine vasopressin modified at position 2 with proline derivatives: selective antagonists of oxytocin in vitro

  • Dariusz Sobolewski
  • Adam Prahl
  • Jiřina Slaninová
  • Bernard Lammek
Part of the Advances in Experimental Medicine and Biology book series (volume 611)

Introduction

In mammals, arginine vasopressin (AVP) is mainly synthesized and released into the circulation by the magnocellular neurons of the supraoptic and paraventricular hypothalamic nuclei, with axons projecting to the pituitary [1]. Physiological effects of AVP are mediated by at least three distinct vasopressin receptor subtypes: V1a, known to mediate the contractile action of AVP on vascular smooth muscles and stimulate glycogenolysis in the liver; V1b (V3), involved in the release of ACTH from pituitary; and V2, receptors mediating antidiuretic action in the kidney [2]. AVP also interacts with oxytocin (OT) receptors which are responsible for the galactobolic and uterotonic effects [3].

Many of the arginine vasopressin (AVP) agonists and antagonists have been designed and synthesized in the course of extensive investigations of the structure — activity relationships [4,5]. All these efforts resulted in probably the best understanding of the relationships among peptide...

Keywords

Peptide Hormone Arginine Vasopressin Hypothalamic Nucleus Vasopressin Receptor Pharmacological Evaluation 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Notes

Acknowledgments

Partial funding for this work was provided by Polish Ministry of Education and Science under Grant No. 0066/H03/2006/30 and 1312/T09/2005/29 and by research project No. Z4055905 of the Academy of Sciences of the Czech Republic.

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Copyright information

© Springer Science+Business Media, LLC 2009

Authors and Affiliations

  • Dariusz Sobolewski
    • 1
  • Adam Prahl
    • 1
  • Jiřina Slaninová
    • 2
  • Bernard Lammek
    • 1
  1. 1.University of GdańskFaculty of ChemistryGdańskPoland
  2. 2.Institute of Organic Chemistry and BiochemistryAcademy of Sciences of the Czech RepublicPragueCzech Republic

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