针对δ-阿片受体的反义寡脱氧核苷酸可选择性阻断小鼠中由δ-阿片受体激动剂而非μ-或κ-阿片受体激动剂诱导的脊髓镇痛作用。
Antisense oligodeoxynucleotide to a delta-opioid receptor selectively blocks the spinal antinociception induced by delta-, but not mu- or kappa-opioid receptor agonists in the mouse.
作者信息
Tseng L F, Collins K A, Kampine J P
机构信息
Department of Anesthesiology, Medical College of Wisconsin, Milwaukee 53226.
出版信息
Eur J Pharmacol. 1994 Jun 2;258(1-2):R1-3. doi: 10.1016/0014-2999(94)90072-8.
An antisense oligodeoxynucleotide (A-oligo) to delta-opioid receptor mRNA was utilized to block the expression of mouse delta-opioid receptor in the spinal cord of male ICR mice. Intrathecal treatment with A-oligo (1.6-163 pmol) dose-dependently attenuated the antinociception induced by i.t. administered DPDPE ([D-Pen2,5]enkephalin) or [D-Ala2]deltorphin II, delta-opioid receptor agonist, without affecting the antinociception induced by DAMGO ([D-Ala2-MePhe4,Gly(ol)5]enkephalin) or U50,488H, respective mu- or kappa-opioid receptor agonists. Scrambled sense oligodeoxynucleotide (163 pmol) was ineffective against the tail-flick inhibition induced by DPDPE,[D-Ala2]deltorphin, DAMGO or U50,488H. The studies confirm previous pharmacological studies at the molecular level indicating a distinct delta-opioid receptor for antinociception in the spinal cord.
利用针对δ-阿片受体mRNA的反义寡脱氧核苷酸（A-oligo）来阻断雄性ICR小鼠脊髓中δ-阿片受体的表达。鞘内注射A-oligo（1.6 - 163 pmol）剂量依赖性地减弱了鞘内注射DPDPE（[D- Pen2,5]脑啡肽）或[D-Ala2]强啡肽II（δ-阿片受体激动剂）所诱导的镇痛作用，而不影响DAMGO（[D-Ala2-MePhe4,Gly(ol)5]脑啡肽）或U50,488H（分别为μ-或κ-阿片受体激动剂）所诱导的镇痛作用。乱序正义寡脱氧核苷酸（163 pmol）对DPDPE、[D-Ala2]强啡肽、DAMGO或U50,488H所诱导的甩尾抑制无效。这些研究在分子水平上证实了先前的药理学研究，表明脊髓中存在用于镇痛的独特δ-阿片受体。
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