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Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats.
Psychopharmacology (Berl). 2007 Jul; 193(1):97-105.P

Abstract

RATIONALE

Tramadol (1RS, 2RS)-2-[(dimethylamino)-methyl]-1-(3-methoxyphenyl)-cyclohexanol) is an atypical centrally acting analgesic agent with weak opioid receptor affinity that, like some antidepressants, enhances the extraneuronal concentrations of the monoamine neurotransmitters, noradrenaline and serotonin, by interfering with their re-uptake and release mechanisms.

OBJECTIVES

The present study was undertaken to evaluate the potential role of 5-HT(1A) receptors and opioids receptors in the analgesic effect of tramadol in neuropathic pain. With this aim, the effect of either a selective 5-HT(1A) receptor antagonist (WAY-100635, N-2-[4-(2-methoxyphenyl-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexane carboxamide) or a selective 5-HT(1A) receptor agonist (8-OH-DPAT, 8-hydroxy-2-(di-n-propylamine) tetralin hydrobromide) or an opioid receptor antagonist (naloxone; naloxone hydrochloride dihydrate) was investigated in combination with tramadol by means of the cold-plate test in the chronic constriction injury model in rats.

RESULTS

The results showed that WAY-100635 (0.8 mg/kg) significantly enhanced the antiallodynic effect of non-effective doses of tramadol (5-10 mg/kg). In contrast, 8-OH-DPAT (0.5 mg/kg) counteracted the antiallodynic effect of an effective dose of tramadol (22 mg/kg). Naloxone (0.5 mg/kg) partially counteracted the antiallodynic effect of tramadol (22 mg/kg).

CONCLUSIONS

These findings suggest the involvement of opioid and 5-HT(1A) receptors in the antinociceptive effect of tramadol and support the idea that the combination of tramadol with compounds having 5-HT(1A) antagonist properties could be a new strategy to improve tramadol-induced analgesia in neuropathic pain.

Authors+Show Affiliations

Pharmacology and Neuroscience Research Group, Department of Neuroscience (Pharmacology and Psychiatry), School of Medicine, University of Cádiz, Plaza Falla 9, 11003, Cadiz, Spain, juanantonio.mico@uca.es.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17393145

Citation

Berrocoso, Esther, et al. "Role of Serotonin 5-HT1A and Opioid Receptors in the Antiallodynic Effect of Tramadol in the Chronic Constriction Injury Model of Neuropathic Pain in Rats." Psychopharmacology, vol. 193, no. 1, 2007, pp. 97-105.
Berrocoso E, De Benito MD, Mico JA. Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats. Psychopharmacology (Berl). 2007;193(1):97-105.
Berrocoso, E., De Benito, M. D., & Mico, J. A. (2007). Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats. Psychopharmacology, 193(1), 97-105.
Berrocoso E, De Benito MD, Mico JA. Role of Serotonin 5-HT1A and Opioid Receptors in the Antiallodynic Effect of Tramadol in the Chronic Constriction Injury Model of Neuropathic Pain in Rats. Psychopharmacology (Berl). 2007;193(1):97-105. PubMed PMID: 17393145.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats. AU - Berrocoso,Esther, AU - De Benito,M Dolores, AU - Mico,Juan A, Y1 - 2007/03/29/ PY - 2006/10/17/received PY - 2007/02/28/accepted PY - 2007/3/30/pubmed PY - 2007/9/7/medline PY - 2007/3/30/entrez SP - 97 EP - 105 JF - Psychopharmacology JO - Psychopharmacology (Berl) VL - 193 IS - 1 N2 - RATIONALE: Tramadol (1RS, 2RS)-2-[(dimethylamino)-methyl]-1-(3-methoxyphenyl)-cyclohexanol) is an atypical centrally acting analgesic agent with weak opioid receptor affinity that, like some antidepressants, enhances the extraneuronal concentrations of the monoamine neurotransmitters, noradrenaline and serotonin, by interfering with their re-uptake and release mechanisms. OBJECTIVES: The present study was undertaken to evaluate the potential role of 5-HT(1A) receptors and opioids receptors in the analgesic effect of tramadol in neuropathic pain. With this aim, the effect of either a selective 5-HT(1A) receptor antagonist (WAY-100635, N-2-[4-(2-methoxyphenyl-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexane carboxamide) or a selective 5-HT(1A) receptor agonist (8-OH-DPAT, 8-hydroxy-2-(di-n-propylamine) tetralin hydrobromide) or an opioid receptor antagonist (naloxone; naloxone hydrochloride dihydrate) was investigated in combination with tramadol by means of the cold-plate test in the chronic constriction injury model in rats. RESULTS: The results showed that WAY-100635 (0.8 mg/kg) significantly enhanced the antiallodynic effect of non-effective doses of tramadol (5-10 mg/kg). In contrast, 8-OH-DPAT (0.5 mg/kg) counteracted the antiallodynic effect of an effective dose of tramadol (22 mg/kg). Naloxone (0.5 mg/kg) partially counteracted the antiallodynic effect of tramadol (22 mg/kg). CONCLUSIONS: These findings suggest the involvement of opioid and 5-HT(1A) receptors in the antinociceptive effect of tramadol and support the idea that the combination of tramadol with compounds having 5-HT(1A) antagonist properties could be a new strategy to improve tramadol-induced analgesia in neuropathic pain. SN - 0033-3158 UR - https://www.unboundmedicine.com/medline/citation/17393145/Role_of_serotonin_5_HT1A_and_opioid_receptors_in_the_antiallodynic_effect_of_tramadol_in_the_chronic_constriction_injury_model_of_neuropathic_pain_in_rats_ L2 - https://dx.doi.org/10.1007/s00213-007-0761-8 DB - PRIME DP - Unbound Medicine ER -