Role of catecholamines and serotonin receptor subtypes in nefopam-induced antinociception
| Autor: | Jean-Marie Gillardin, Philippe Girard, Yannick Pansart, Danielle Verniers, Marie-Claude Coppé |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Male
medicine.medical_specialty Ketanserin Serotonin 5-HT1 Receptor Antagonists Pharmacology Serotonergic Mice Catecholamines Nefopam Internal medicine medicine Prazosin Serotonin 5-HT2 Receptor Antagonists Animals Biogenic Monoamines Drug Interactions Adrenergic alpha-Antagonists 5-HT receptor Mice Inbred ICR Chemistry Receptors Dopamine D1 Adrenergic alpha-2 Receptor Antagonists Nociceptors Analgesics Non-Narcotic Rats Yohimbine Endocrinology Receptors Serotonin Adrenergic alpha-1 Receptor Antagonists Dopamine Antagonists Serotonin Antagonists medicine.drug |
| Zdroj: | Pharmacological Research. 54:195-202 |
| ISSN: | 1043-6618 |
| DOI: | 10.1016/j.phrs.2006.04.008 |
| Popis: | The non-opiate analgesic nefopam has been shown to inhibit monoamines uptake, but little is known about receptor subtypes effectively involved in its analgesic effect. In vitro binding assays yielded the following measures of affinity (IC(50)): serotonergic 5-HT(2C) (1.4 microM), 5-HT(2A) (5.1 microM), 5-HT(3) (22.3 microM), 5-HT(1B) (41.7 microM), 5-HT(1A) (64.9 microM), adrenergic alpha(1) (15.0 microM) and dopaminergic D(1) (100 microM). Subcutaneous nefopam administration dose-dependently inhibited pain in acetic acid-induced writhing (1-30 mg kg(-1)) and formalin (1-10 mg kg(-1)) tests in the mouse. Pretreatments with adrenergic alpha(1) (prazosin) and alpha(2) (yohimbine), and serotonergic 5-HT(1B) (GR127935) receptor antagonists significantly increased the nefopam ED(50) in the writhing test. The serotonergic 5-HT(2C) (RS102221) and the dopaminergic D(2) (sulpiride) receptor antagonists inhibited nefopam antinociception in the formalin test. However, in both tests, nefopam analgesic activity was not modified by the following receptor antagonists: dopaminergic D(1) (SCH23390), serotonergic 5-HT(1A) (NAN-190, WAY100635), 5-HT(2A) (R96544, ketanserin), 5-HT(3) (tropisetron), and 5-HT(4) (SDZ205557). In conclusion, nefopam analgesic activity could be modulated by the adrenergic alpha(1) and alpha(2) receptors, the dopaminergic D(2) receptors, and the serotonergic 5-HT(1B) and 5-HT(2C) receptor subtypes. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect