Literature DB >> 6688

Use of the mouse jumping test for estimating antagonistic potencies of morphine antagonists.

A Cowan.   

Abstract

The potencies of 19 reference morphine antagonists have been compared in a modified version of the mouse jumping test. Mice were each implanted subcutaneously with one 75 mg pellet of morphine. Antagonist challenge took place 72 h later and the incidence of repetitive vertical-jumping was monitored over 1 h. A high Pearson correlation coefficient (r = 0.997) was found between quantitative assays based on the total number of jumps per mouse and quantal assays based on mice jumping at least 6 times. A comparison of relative potencies obtained with the mouse test and with non-withdrawn morphine-dependent monkeys gave a Spearman rank order coefficient of 0.91 while a similar comparison with values obtained with the guinea-pig isolated ileum preparation also gave a high correlation coefficient (r= 0.92). Whereas it is difficult to assess the antagonistic component of buprenorphine and cyclorphan with the ileum preparation, both compounds can be satisfactorily assayed in the mouse jumping test. The reported antagonistic properties of ketocyclazocine and profadol could not be confirmed in the mouse model.

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Year:  1976        PMID: 6688     DOI: 10.1111/j.2042-7158.1976.tb04126.x

Source DB:  PubMed          Journal:  J Pharm Pharmacol        ISSN: 0022-3573            Impact factor:   3.765


  8 in total

1.  Mixed agonist-antagonist opiates and physical dependence.

Authors:  J J Jacob; G M Michaud; E C Tremblay
Journal:  Br J Clin Pharmacol       Date:  1979       Impact factor: 4.335

2.  Opioid antagonists differ according to negative intrinsic efficacy in a mouse model of acute dependence.

Authors:  Ellen A Walker; Steven N Sterious
Journal:  Br J Pharmacol       Date:  2005-08       Impact factor: 8.739

3.  Buprenorphine: a unique drug with complex pharmacology.

Authors:  Kabirullah Lutfy; Alan Cowan
Journal:  Curr Neuropharmacol       Date:  2004-10       Impact factor: 7.363

Review 4.  Buprenorphine: a review of its pharmacological properties and therapeutic efficacy.

Authors:  R C Heel; R N Brogden; T M Speight; G S Avery
Journal:  Drugs       Date:  1979-02       Impact factor: 9.546

5.  Diprenorphine and naloxone in squirrel monkeys with enhanced sensitivity to opioid antagonists.

Authors:  A H Oliveto; L A Dykstra
Journal:  Psychopharmacology (Berl)       Date:  1988       Impact factor: 4.530

6.  Agonist and antagonist properties of buprenorphine, a new antinociceptive agent.

Authors:  A Cowan; J W Lewis; I R Macfarlane
Journal:  Br J Pharmacol       Date:  1977-08       Impact factor: 8.739

7.  Threshold differences for naloxone and naltrexone in the hypothalamus and midbrain using fixed ratio brain self-stimulation in rats.

Authors:  G J Schaefer; R P Michael
Journal:  Psychopharmacology (Berl)       Date:  1981       Impact factor: 4.530

Review 8.  Nalbuphine. A preliminary review of its pharmacological properties and therapeutic efficacy.

Authors:  J K Errick; R C Heel
Journal:  Drugs       Date:  1983-09       Impact factor: 9.546

  8 in total

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