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The analgesic efficacy of partial opioid agonists is increased in mice with targeted inactivation of the alpha2A-adrenoceptor gene.

Abstract：

:Alpha(2A)-Adrenoceptors mediate the antinociceptive effects of alpha(2)-adrenoceptor agonists in mice, and analgesic synergism between noradrenergic and opioidergic mechanisms has been reported to be lacking in mice devoid of functional alpha(2A)-adrenoceptors. We investigated whether the antinociceptive actions of opioid agonists with different efficacy would be altered in mice with targeted inactivation of the alpha(2A)-adrenoceptor gene (alpha(2A)-KO mice). The antinociceptive effects of fentanyl, morphine, buprenorphine and tramadol were assessed using conventional tail-flick and hot-plate assays. Antinociceptive responses to fentanyl were unaltered in the alpha(2A)-KO animals. Morphine analgesia was slightly accentuated in the tail-flick test. The naloxone-sensitive antinociceptive responses to both tested weak partial agonists were very markedly accentuated in both tests. For example, after 40 mg/kg tramadol administration, the tramadol-induced prolongation of tail-flick latency was 86+/-6% of the maximal possible effect (MPE) in alpha(2A)-KO and 22+/-2% of MPE in control mice; prolongation of hot-plate latency was 93+/-5% of MPE in alpha(2A)-KO mice and 8+/-2% of MPE in the controls (P<0.001 for both). The effects of alpha(2A)-KO were mimicked by pretreatment of wild-type control mice with the alpha(2)-adrenoceptor antagonists, atipamezole and yohimbine; the apparent efficacy of tramadol and buprenorphine now approached that of morphine and fentanyl. Other behavioural effects of the tested opioid agonists were not similarly influenced by alpha(2A)-KO. Antagonists of alpha(2A)-adrenoceptors may offer a novel mechanism to augment the antinociceptive actions of partial opioid agonists.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Ozdoğan UK,Lähdesmäki J,Scheinin M

doi

10.1016/j.ejphar.2005.10.029

keywords:

subject

Has Abstract

pub_date

2006-01-04 00:00:00

pages

105-13

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(05)01095-2

journal_volume

529

pub_type

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