Literature DB >> 7202521

Analgesic properties of the GABA-mimetic THIP.

R C Hill, R Maurer, H H Buescher, D Roemer.   

Abstract

The analgesic properties of the muscimol analogue THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) in laboratory animals were compared with those of baclofen, morphine and muscimol. THIP was active orally and parenterally and resembled muscimol qualitatively in its actions. Quantitatively, THIP and baclofen were 2--3 times less potent than morphine and 5--15 times less potent than muscimol. The analgesic effects of THIP, baclofen and muscimol were not reversed by naloxone or bicuculline.

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Year:  1981        PMID: 7202521     DOI: 10.1016/0014-2999(81)90419-2

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN: 0014-2999            Impact factor:   4.432


  14 in total

1.  Modulation of spinal GABAergic analgesia by inhibition of chloride extrusion capacity in mice.

Authors:  Marina N Asiedu; Galo Mejia; Michael K Ossipov; T Phillip Malan; Kai Kaila; Theodore J Price
Journal:  J Pain       Date:  2012-04-25       Impact factor: 5.820

Review 2.  GABA pharmacology: the search for analgesics.

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

3.  Intracisternal or intrathecal glycine, taurine, or muscimol inhibit bicuculline-induced allodynia and thermal hyperalgesia in mice.

Authors:  Il-ok Lee; Eui-sung Lim
Journal:  Acta Pharmacol Sin       Date:  2010-08       Impact factor: 6.150

4.  The analgesic effect of the GABA-agonist THIP in patients with chronic pain of malignant origin. A phase-1-2 study.

Authors:  M Kjaer; H Nielsen
Journal:  Br J Clin Pharmacol       Date:  1983-11       Impact factor: 4.335

5.  Inhibition of substance P release is the key to successful management of oral pain.

Authors:  D B Goodale
Journal:  Anesth Prog       Date:  1982 Jul-Aug

6.  Effects of GABAergic drugs on the GABA turnover in the substantia nigra and the corpus striatum of the rat.

Authors:  S Lindgren
Journal:  J Neural Transm       Date:  1987       Impact factor: 3.575

7.  Estradiol and testosterone modulate the anesthetic action of the GABA-A agonist THIP, but not of the neurosteroid 3alpha,5beta-pregnanolone in the rat.

Authors:  Oscar González-Flores; Norma Sánchez; Marcos García-Juárez; Francisco Javier Lima-Hernández; Gabriela González-Mariscal; Carlos Beyer
Journal:  Psychopharmacology (Berl)       Date:  2003-12-17       Impact factor: 4.530

Review 8.  Pharmacodynamic effects and possible therapeutic uses of THIP, a specific GABA-agonist.

Authors:  A V Christensen; O Svendsen; P Krogsgaard-Larsen
Journal:  Pharm Weekbl Sci       Date:  1982-10-22

9.  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

10.  Periaqueductal gray matter involvement in the muscimol-induced decrease of morphine antinociception.

Authors:  F Zambotti; N Zonta; M Parenti; R Tommasi; L Vicentini; F Conci; P Mantegazza
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1982-03       Impact factor: 3.000

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