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Role of catecholamines and serotonin receptor subtypes in nefopam-induced antinociception.
Pharmacol Res. 2006 Sep; 54(3):195-202.PR

Abstract

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.

Authors+Show Affiliations

Biocodex, Service de Pharmacologie, Zac de Mercières 60200 Compiègne, France.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16750379

Citation

Girard, Philippe, et al. "Role of Catecholamines and Serotonin Receptor Subtypes in Nefopam-induced Antinociception." Pharmacological Research, vol. 54, no. 3, 2006, pp. 195-202.
Girard P, Coppé MC, Verniers D, et al. Role of catecholamines and serotonin receptor subtypes in nefopam-induced antinociception. Pharmacol Res. 2006;54(3):195-202.
Girard, P., Coppé, M. C., Verniers, D., Pansart, Y., & Gillardin, J. M. (2006). Role of catecholamines and serotonin receptor subtypes in nefopam-induced antinociception. Pharmacological Research, 54(3), 195-202.
Girard P, et al. Role of Catecholamines and Serotonin Receptor Subtypes in Nefopam-induced Antinociception. Pharmacol Res. 2006;54(3):195-202. PubMed PMID: 16750379.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Role of catecholamines and serotonin receptor subtypes in nefopam-induced antinociception. AU - Girard,Philippe, AU - Coppé,Marie-Claude, AU - Verniers,Danielle, AU - Pansart,Yannick, AU - Gillardin,Jean-Marie, Y1 - 2006/05/04/ PY - 2006/03/08/received PY - 2006/04/19/revised PY - 2006/04/20/accepted PY - 2006/6/6/pubmed PY - 2006/10/6/medline PY - 2006/6/6/entrez SP - 195 EP - 202 JF - Pharmacological research JO - Pharmacol Res VL - 54 IS - 3 N2 - 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. SN - 1043-6618 UR - https://www.unboundmedicine.com/medline/citation/16750379/Role_of_catecholamines_and_serotonin_receptor_subtypes_in_nefopam_induced_antinociception_ DB - PRIME DP - Unbound Medicine ER -