Literature DB >> 3017490

Meptazinol has a similar agonist action on opioid receptors in field-stimulated mouse vas deferens and guinea-pig ileum.

J Goodall, I E Hughes, D Mackay.   

Abstract

The effects of the opioid receptor agonist RX783006 and of the opioid receptor partial agonist (+)-meptazinol have been examined on electrically induced twitch responses of the guinea-pig isolated ileum and of the mouse isolated vas deferens. Log10 concentration-tissue state curves were determined for (+)-meptazinol and RX783006, alone, in combination and in the presence of naloxone (30 nM). Analysis of these log10 concentration-tissue state curves using the null equations derived and tested in the preceding paper indicates that the opioid agonist action of (+)-meptazinol on mouse vas deferens is quantitatively similar to that on guinea-pig ileum. The results also suggest that (+)-meptazinol acts as a functional antagonist on the guinea-pig ileum as well as on the mouse vas deferens. The potency of (+)-meptazinol relative to RX783006 has been measured by an indirect method which should eliminate any functional antagonistic action of (+)-meptazinol. This method gives a relative potency of (+)-meptazinol in both tissues which is three to six times greater than that measured directly on guinea-pig ileum. This discrepancy may be due to experimental error but it may also indicate that direct measurements on guinea-pig ileum underestimate the agonist potency of this compound on opioid receptors.

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Year:  1986        PMID: 3017490      PMCID: PMC1916985          DOI: 10.1111/j.1476-5381.1986.tb10246.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  7 in total

1.  The pharmacological classification of practolol and chloropractolol.

Authors:  T P Kenakin; J W Black
Journal:  Mol Pharmacol       Date:  1978-07       Impact factor: 4.436

2.  Similarity between mu-opioid receptors in mouse vas deferens and guinea-pig ileum.

Authors:  J Goodall; I E Hughes; D Mackay
Journal:  Br J Pharmacol       Date:  1985-05       Impact factor: 8.739

3.  Quantification of the actions of agonists that simultaneously act on a particular type of receptor and have separate functional interactant properties.

Authors:  J Goodall; I E Hughes; D Mackay
Journal:  Br J Pharmacol       Date:  1986-07       Impact factor: 8.739

4.  Difference between mu-receptors in the guinea pig ileum and the mouse vas deferens.

Authors:  L M Sayre; P S Portoghese; A E Takemori
Journal:  Eur J Pharmacol       Date:  1983-05-20       Impact factor: 4.432

5.  Quantification of the characteristics of antagonists exhibiting both competitive antagonism and functional interaction.

Authors:  I E Hughes; D Mackay
Journal:  Br J Pharmacol       Date:  1985-05       Impact factor: 8.739

6.  A general analysis of the receptor-drug interaction.

Authors:  D Mackay
Journal:  Br J Pharmacol Chemother       Date:  1966-01

7.  Pharmacological effects of meptazinol and its enantiomers on guinea-pig ileum and mouse vas deferens.

Authors:  R J Duchesne; J Goodall; I E Hughes
Journal:  J Pharm Pharmacol       Date:  1984-08       Impact factor: 3.765

  7 in total

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