Literature DB >> 6319887

Opiate receptors in the rat vas deferens.

C F Smith, M J Rance.   

Abstract

The nature of the opiate receptor population in the rat vas deferens (RVD) has been examined by evaluating the interaction of a range of antagonists with prototypic mu-, kappa- and sigma-opioid agonists in the tissue. Ke values for 5 antagonists against normorphine in the isolated mouse vas deferens showed excellent correlation with Ke values obtained against the mu-agonist RX783030 in the RVD. RX783030 could be effectively antagonised by naltrexone in the RVD but not by the sigma-antagonist ICI 154129 whereas D-Ala2,D-Leu5-enkephalin required both antagonists to yield parallel shifts of its dose response. The lack of agonist activity of morphine is a result of the low intrinsic activity of this agent in the RVD. The kappa-agonists ethylketocyclazocine, tifluadom and U50488 also showed antagonist properties in the RVD. These results can be rationalised by postulating that the RVD contains a mu-receptor population with a high intrinsic activity requirement together with some sigma-receptors. It is not necessary to propose the existence of a novel epsilon-receptor in order to rationalise the data reported.

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Year:  1983        PMID: 6319887     DOI: 10.1016/0024-3205(83)90509-x

Source DB:  PubMed          Journal:  Life Sci        ISSN: 0024-3205            Impact factor:   5.037


  9 in total

1.  Differential sensitivity of models of antinociception in the rat, mouse and guinea-pig to mu- and kappa-opioid receptor agonists.

Authors:  A G Hayes; M J Sheehan; M B Tyers
Journal:  Br J Pharmacol       Date:  1987-08       Impact factor: 8.739

Review 2.  Efficacy and ligand bias at the μ-opioid receptor.

Authors:  E Kelly
Journal:  Br J Pharmacol       Date:  2013-08       Impact factor: 8.739

3.  The contributions of mu-, delta- and kappa-opioid receptors to the actions of endogenous opioids on spinal reflexes in the rabbit.

Authors:  R W Clarke; T W Ford
Journal:  Br J Pharmacol       Date:  1987-07       Impact factor: 8.739

4.  Beta-endorphin-sensitive opioid receptors in the rat tail artery.

Authors:  P Illes; R Bettermann; I Brod; B Bucher
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-04       Impact factor: 3.000

5.  The physiological relevance of low agonist affinity binding at opioid mu-receptors.

Authors:  J A Carroll; J S Shaw; A D Wickenden
Journal:  Br J Pharmacol       Date:  1988-06       Impact factor: 8.739

6.  Opioid receptor characterisation of neuronally stimulated isolated human vas deferens.

Authors:  James Root; Ana Monica Lopes Correia Wakenhut; Holly Siggins; Sidath Katugampola; Carolyn Napier
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2012-06-15       Impact factor: 3.000

7.  The contribution of intrinsic activity to the action of opioids in vitro.

Authors:  L Miller; J S Shaw; E M Whiting
Journal:  Br J Pharmacol       Date:  1986-03       Impact factor: 8.739

8.  Alkylation with beta-funaltrexamine suggests differences between mu-opioid receptor systems in guinea-pig brain and myenteric-plexus.

Authors:  T G Franklin; J R Traynor
Journal:  Br J Pharmacol       Date:  1991-03       Impact factor: 8.739

9.  On the opioid receptor subtype inhibiting the evoked release of 3H-noradrenaline from guinea-pig atria in vitro.

Authors:  H Fuder; M Buder; H D Riers; G Rothacher
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-02       Impact factor: 3.000

  9 in total

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