Potentiation of Morphine Analgesia by Adjuvant Activation of 5-HT7 Receptors
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- Brenchat Alex
- Department of Pharmacology, Drug Discovery and Preclinical Development, Esteve, Spain
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- Ejarque Miriam
- Department of Pharmacology, Drug Discovery and Preclinical Development, Esteve, Spain
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- Zamanillo Daniel
- Department of Pharmacology, Drug Discovery and Preclinical Development, Esteve, Spain
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- Vela José Miguel
- Department of Pharmacology, Drug Discovery and Preclinical Development, Esteve, Spain
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- Romero Luz
- Department of Pharmacology, Drug Discovery and Preclinical Development, Esteve, Spain
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Abstract
Spinal blockade of 5-HT7 receptors has been reported to inhibit the antinociceptive effect of opioids. In this study, we found that subcutaneous administration of the selective 5-HT7 receptor agonist E-55888 (10 mg/kg) or the antagonist SB-258719 (5 mg/kg) exerted no effect on the tail-flick test in mice. However, E-55888, but not SB-258719, increased (2.6-fold) the analgesic potency of oral morphine. The potentiating effect exerted by E-55888 was prevented by SB-258719. A pharmacokinetic interaction was discarded as morphine plasma and brain concentrations were not significantly modified when co-administered with E-55888. These results reinforce the involvement of 5-HT7 receptors in opioid analgesia and point to a potential use of 5-HT7 receptor agonists as adjuvants of opioid analgesia.
Journal
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- Journal of Pharmacological Sciences
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Journal of Pharmacological Sciences 116 (4), 388-391, 2011
The Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390282680155079296
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- NII Article ID
- 10029895708
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- NII Book ID
- AA11806667
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- ISSN
- 13478648
- 13478613
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- NDL BIB ID
- 11206996
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- PubMed
- 21778664
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed