Literature DB >> 886473

The analgesic action of baclofen [beta-(4-chlorophenyl)-gamma-aminobutyric acid].

R A Levy, H K Proudfit.   

Abstract

When administered to mice, baclofen induced dose-related antinocisponsive activity in the stretch, hot plate and tail-flick tests. Although high doses also impaired motor coordination, as measured by the rotating rod test, the following observations suggest that the pronounced antinocisponsive effect of higher doses did not reflect a reduced capacity to respond to perceived pain: motor impairment, having shorter onset of action, was fully developed before the appearance of any analgesic action; mice made completely tolerant to the motor effect were still analgesic; and other agents which severely impaired rotating rod performance did not necessarily show antinocisponsive activity in the hot plate test. The mechanism of action of baclofen is not similar to that of morphine since naloxone did not antagonize the analgesic effect of baclofen, and cross-tolerance between morphine- and baclofen-induced analgesia could not be demonstrated.

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Year:  1977        PMID: 886473

Source DB:  PubMed          Journal:  J Pharmacol Exp Ther        ISSN: 0022-3565            Impact factor:   4.030


  15 in total

1.  Chronic baclofen desensitizes GABA(B)-mediated G-protein activation and stimulates phosphorylation of kinases in mesocorticolimbic rat brain.

Authors:  Bradley M T Keegan; Thomas J R Beveridge; Jeffrey J Pezor; Ruoyu Xiao; Tammy Sexton; Steven R Childers; Allyn C Howlett
Journal:  Neuropharmacology       Date:  2015-02-25       Impact factor: 5.250

2.  The differential effects of baclofen on segmental and descending excitation of spinal interneurones in the cat.

Authors:  D R Curtis; R Malik
Journal:  Exp Brain Res       Date:  1985       Impact factor: 1.972

Review 3.  GABA pharmacology: the search for analgesics.

Authors:  Kenneth E McCarson; S J Enna
Journal:  Neurochem Res       Date:  2014-02-15       Impact factor: 3.996

Review 4.  Spasticity and drug therapy.

Authors:  E W Wuis
Journal:  Pharm Weekbl Sci       Date:  1987-10-16

5.  Regulators of G-Protein Signaling (RGS) Proteins Promote Receptor Coupling to G-Protein-Coupled Inwardly Rectifying Potassium (GIRK) Channels.

Authors:  Kylie B McPherson; Emily R Leff; Ming-Hua Li; Claire Meurice; Sherrica Tai; John R Traynor; Susan L Ingram
Journal:  J Neurosci       Date:  2018-08-27       Impact factor: 6.167

6.  Ketogenic diets and thermal pain: dissociation of hypoalgesia, elevated ketones, and lowered glucose in rats.

Authors:  David N Ruskin; Tracey A C S Suter; Jessica L Ross; Susan A Masino
Journal:  J Pain       Date:  2013-03-15       Impact factor: 5.820

7.  Monoamines as mediators of the antinociceptive effect of baclofen.

Authors:  J Sawynok
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1983-06       Impact factor: 3.000

8.  CGP 35348, a new GABAB antagonist, prevents antinociception and muscle-relaxant effect induced by baclofen.

Authors:  M Malcangio; C Ghelardini; A Giotti; P Malmberg-Aiello; A Bartolini
Journal:  Br J Pharmacol       Date:  1991-06       Impact factor: 8.739

9.  Hyperpolarization by GABAB receptor agonists in mid-brain periaqueductal gray neurones in vitro.

Authors:  B Chieng; M J Christie
Journal:  Br J Pharmacol       Date:  1995-09       Impact factor: 8.739

10.  GABAA-benzodiazepine receptor availability in smokers and nonsmokers: relationship to subsyndromal anxiety and depression.

Authors:  Irina Esterlis; Kelly P Cosgrove; Jeffery C Batis; Frederic Bois; Tracy A Kloczynski; Stephanie M Stiklus; Edward Perry; Gilles D Tamagnan; John P Seibyl; Robert Makuch; Suchitra Krishnan-Sarin; Stephanie O'Malley; Julie K Staley
Journal:  Synapse       Date:  2009-12       Impact factor: 2.562

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