Dual allosteric modulation of opioid antinociceptive potency by α2A-adrenoceptors
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- 作者：Anne-Julie Chabot-Doré ; a ; b ; 1 ; anne-julie.chabot-dore@mail.mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Magali Millecampsa ; c ; 2 ; magali.millecamps@mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Lina Nasoa ; c ; 2 ; lina.naso@mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Dominic Devoste ; 3 ; dominic.devost@mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Phan Trieue ; 3 ; phan.trieu@mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Marjo Piltonena ; c ; 1 ; marjo.piltonen@mail.mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Luda Diatchenkoa ; c ; d ; 1 ; luda.diatchenko@mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Carolyn A. Fairbanksf ; g ; h ; 4 ; carfair@umn.edu" class="auth_mail" title="E-mail the corresponding author ; George L. Wilcoxg ; h ; i ; 4 ; george@umn.edu" class="auth_mail" title="E-mail the corresponding author ; Terence E. Hé ; berte ; 3 ; terence.hebert@mcgill.ca" class="auth_mail" title="E-mail the corresponding author ; Laura S. Stonea ; b ; c ; d ; e ; laura.s.stone@mcgill.ca" class="auth_mail" title="E-mail the corresponding author
- 关键词：α2-adrenoceptor ; Opioid receptor ; Norepinephrine ; Spinal cord ; Morphine ; Analgesia
- 刊名：Neuropharmacology
- 出版年：2015
- 出版时间：December 2015
- 年：2015
- 卷：99
- 期：Complete
- 页码：285-300
- 全文大小：2365 K
文摘
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The role of α2A-adrenoceptors (ARs) in spinal opioid antinociception was investigated.
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The α2A-AR is necessary for analgesic synergy between clonidine and opioid agonists.
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Opioid antinociception is enhanced in α2A-AR-KO mice.
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A model of activation state-dependent allosteric modulation is proposed.
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The model has implications for allosteric modulation of other G protein-coupled receptor pairs.