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Significance of GABAergic systems in the action of improgan, a non-opioid analgesic
- Source :
- Hough, L H, Nalwalk, J B, Leurs, R, Menge, W M P B & Timmerman, H 2001, ' Significance of GABAergic systems in the action of improgan, a non-opioid analgesic ', Life Sciences, vol. 68, no. 24, pp. 2751-7 . https://doi.org/10.1016/S0024-3205(01)01080-3, Life Sciences, 68(24), 2751-7. Elsevier Inc.
- Publication Year :
- 2001
-
Abstract
- Improgan is the prototype drug from a new class of non-opioid analgesics chemically related to histamine and histamine antagonists, but the mechanism of action of these compounds has not been identified. Because several classes of analgesics act in the brain by reducing GABAergic inhibition of endogenous pain-relieving circuits, and because the activity of these substances is abolished by the GABA(A) agonist muscimol, the present study assessed the effects of muscimol on improgan antinociception in rats. Intracerebroventricular (icv) improgan (80 microg) and morphine (20 microg) both induced 80-100% of maximal analgesic responses on the tail flick test 10 to 30 min later. However, muscimol pretreatment (0.5 microg, icv) completely eliminated the antinociceptive activity of both compounds. Since improgan in vitro lacks activity at opioid and GABA(A) receptors, these findings: 1) confirm earlier literature showing that muscimol inhibits morphine analgesia, and 2) suggest that improgan activates a supraspinal, descending analgesic pathway, possibly via inhibition of GABAergic transmission. Since muscimol is the first compound discovered which inhibits improgan analgesia, muscimol will be a useful tool for the further characterization of this new class of pain-relieving substances.
- Subjects :
- Agonist
Male
medicine.drug_class
Analgesic
Pharmacology
General Biochemistry, Genetics and Molecular Biology
Rats, Sprague-Dawley
chemistry.chemical_compound
SDG 3 - Good Health and Well-being
medicine
Animals
General Pharmacology, Toxicology and Pharmaceutics
gamma-Aminobutyric Acid
Morphine
Chemistry
GABAA receptor
Muscimol
General Medicine
Analgesics, Non-Narcotic
Receptors, GABA-A
Rats
nervous system
Mechanism of action
Opioid
medicine.symptom
Cimetidine
psychological phenomena and processes
Tail flick test
medicine.drug
Subjects
Details
- Language :
- English
- ISSN :
- 00243205
- Database :
- OpenAIRE
- Journal :
- Hough, L H, Nalwalk, J B, Leurs, R, Menge, W M P B & Timmerman, H 2001, ' Significance of GABAergic systems in the action of improgan, a non-opioid analgesic ', Life Sciences, vol. 68, no. 24, pp. 2751-7 . https://doi.org/10.1016/S0024-3205(01)01080-3, Life Sciences, 68(24), 2751-7. Elsevier Inc.
- Accession number :
- edsair.doi.dedup.....e262381581c0efd53c85196487e55b8b