Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain

Daniel Dorsa, M. D. Brot, L. M. Shewey, K. M. Meyers, P. Szot, M. A. Miller

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

The ability of d(CH2)5-Tyr(Me)-arginine-8-vasopressin, an antagonist of peripheral pressoric (V1-type) vasopressin receptors, to label vasopressin binding sites in the septum of the rat brain was evaluated. Using crude membrane preparations from the septum, 3H-arginine-8-vasopressin (AVP) specifically labels a single class of binding sites with a K(d) of 2.9 nM and maximum binding site concentration of 19.8 fmole/mg protein. 3H-Antag also labels a single class of membrane sites but with higher affinity (K(d) = 0.47 nM) and lower capacity (10.1 fmole/mg protein) than 3H-AVP. The rank order of potency of various competitor peptides for 3H-AVP and 3H-Antag binding was similar. Oxytocin was 100-1,000 fold less potent than AVP in competing for binding with both ligands. 3H-AVP and 3H-Antag showed similar labeling patterns when incubated with septal tissue slices. Unlabeled Antag also effectively antagonized vasopressin-stimulated phosphatidylinositol hydrolysis in septal tissue slices.

Original languageEnglish (US)
Pages (from-to)205-211
Number of pages7
JournalSynapse
Volume2
Issue number3
StatePublished - 1988
Externally publishedYes

Fingerprint

Septum of Brain
Vasopressin Receptors
Arginine Vasopressin
Binding Sites
Vasopressins
Membranes
Oxytocin
Phosphatidylinositols
Antidiuretic Hormone Receptor Antagonists
Proteins
Hydrolysis
Ligands
Peptides

ASJC Scopus subject areas

  • Physiology
  • Neuroscience(all)
  • Pharmacology

Cite this

Dorsa, D., Brot, M. D., Shewey, L. M., Meyers, K. M., Szot, P., & Miller, M. A. (1988). Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain. Synapse, 2(3), 205-211.

Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain. / Dorsa, Daniel; Brot, M. D.; Shewey, L. M.; Meyers, K. M.; Szot, P.; Miller, M. A.

In: Synapse, Vol. 2, No. 3, 1988, p. 205-211.

Research output: Contribution to journalArticle

Dorsa, D, Brot, MD, Shewey, LM, Meyers, KM, Szot, P & Miller, MA 1988, 'Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain', Synapse, vol. 2, no. 3, pp. 205-211.
Dorsa D, Brot MD, Shewey LM, Meyers KM, Szot P, Miller MA. Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain. Synapse. 1988;2(3):205-211.
Dorsa, Daniel ; Brot, M. D. ; Shewey, L. M. ; Meyers, K. M. ; Szot, P. ; Miller, M. A. / Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain. In: Synapse. 1988 ; Vol. 2, No. 3. pp. 205-211.
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