Prochlorperazine induces central antinociception mediated by the muscarinic system
| Autor: | Carla Uslenghi, Nicoletta Galeotti, Alessandro Bartolini, Irene Grazioli, Carla Ghelardini |
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| Rok vydání: | 2004 |
| Předmět: |
Agonist
Male medicine.medical_specialty Quinpirole medicine.drug_class (+)-Naloxone Pharmacology Prochlorperazine Mice Internal medicine medicine Animals Pain Measurement Analgesics Acetylcholine antisense oligodeoxynucleotide aODN degenerate oligodeoxynucleotide dODN HC-3 hemicolinium-3 hydrobromide i.c.v i.p intracerebroventricular intraperitoneal M1 muscarinic receptor subtype s.c subcutaneous Dose-Response Relationship Drug Morphine Chemistry Receptors Dopamine D2 Antagonist Muscarinic antagonist Pirenzepine Receptors Muscarinic Dopamine D2 Receptor Antagonists Endocrinology Opioid antagonist medicine.drug |
| Zdroj: | Pharmacological research. 50(3) |
| ISSN: | 1043-6618 |
| Popis: | The antinociceptive effect of the D 2 antagonist prochlorperazine was examined in the mouse hot-plate and abdominal constriction tests. Prochlorperazine (1–2 mg kg −1 s.c./i.p.) produced an increase of the pain threshold in the mouse hot-plate test. The antinociception produced by prochlorperazine was prevented by the D 2 selective agonist quinpirole, the unselective muscarinic antagonist atropine, the M 1 selective antagonist pirenzepine, and by the choline uptake inhibitor hemicholinium-3 hydrobromide (HC-3). Moreover, prochlorperazine antinociception was abolished by pretreatment with an aODN against the M 1 receptor subtype, administered at the dose of 2 nmol per single i.c.v. injection. By contrast the analgesic effect of prochlorperazine was not prevented by the opioid antagonist naloxone and the GABA B antagonist CGP-35348. Prochlorperazine also elicited a dose-dependent increase in ACh release from rat cerebral cortex. In the antinociceptive dose-range, prochlorperazine did not impair mouse performance evaluated by the rota-rod and hole-board tests. On the basis of the above data, it can be postulated that prochlorperazine exerted an antinociceptive effect mediated by a central cholinergic mechanism. |
| Databáze: | OpenAIRE |
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