Analogues of arginine vasopressin modified at position 2 with proline derivatives: selective antagonists of oxytocin in vitro
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 . 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 . AVP also interacts with oxytocin (OT) receptors which are responsible for the galactobolic and uterotonic effects .
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...
KeywordsPeptide Hormone Arginine Vasopressin Hypothalamic Nucleus Vasopressin Receptor Pharmacological Evaluation
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.
- 1.Barberis, C. and Tribollet, E. Crit. Rev. Neurobiol. 10, 119–154 (1996).Google Scholar
- 4.Manning, M. and Sawyer, W. H. J. Receptor Res. 13, 195–214 (1993).Google Scholar
- 5.Lebl, M., Jošt, K. and Brtník, F., In Jošt, K., Lebl, M. and Brtník, F. (Eds.) Handbook of Neurohypophyseal Hormone Analogs, Vol II, Part 2: CRC Press Inc., Boca Raton, Florida, 127–267 (1987).Google Scholar
- 7.Hlavacek, J., In Jošt, K., Lebl, M. and Brtník, F. (Eds.) Handbook of Neurohypophyseal Hormone Analogs, Vol I, Part 2: CRC Press Inc., Boca Raton, Florida, 109–129 (1987).Google Scholar