Activation of spinal delta-1 or delta-2 opioid receptors reduces carrageenan-induced hyperalgesia in the rat.
Activation of spinal delta-1 or delta-2 opioid receptors reduces carrageenan-induced hyperalgesia in the rat.
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发表时间：
1994-02
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通讯作者：
P. Stewart;Donna L. Hammond
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作者：
P. Stewart;Donna L. Hammond
利用角叉菜胶诱导的热痛敏模型研究脊髓δ阿片受体在介导抗伤害感受中的作用。鞘内注射[D-Ala 2，Glu 4]-deltorphin（DELT）（一种delta-2受体激动剂）或DPDPE（一种delta-1受体激动剂）可产生剂量依赖性的爪反射潜伏期（PFL）增加，DELT的ED 50为14.0 μ g，DPDPE为30.4 μ g。DAMGO是一种mu受体激动剂，鞘内给药时也以剂量依赖性方式增加PFL，ED 50为0.02微克。每种阿片类激动剂增加PFL的值，超过基线lavonin注射角叉菜胶之前确定。然而，DELT和DPDPE增加PFL的程度大于DAMGO。同时给予30 μ g纳曲吲哚使DELT的剂量效应线向右偏移3.5倍，使DPDPE的剂量效应线向右偏移2.5倍，这与其作为混合δ-1/δ-2受体拮抗剂的特征一致。同时给予3微克纳曲苯（NTB）使DELT的剂量效应线向右移动3.2倍，而10微克NTB使DELT的剂量效应线向右移动至少15倍。两种剂量的NTB均不能拮抗DPDPE的作用。这些数据与NTB作为选择性δ-2受体拮抗剂的特征一致。DAMGO产生的抗伤害作用可被30 μ g纳曲吲哚非竞争性地拮抗，而被10 μ g NTB竞争性地拮抗。因此，虽然NTB区分δ-1和δ-2阿片受体，但高剂量可能无法有效区分δ和μ受体。（250字处删节）
The role of spinal delta opioid receptors in mediating antinociception was studied by using the carrageenan-induced model of thermal hyperalgesia. Intrathecal administration of [D-Ala2, Glu4]-deltorphin (DELT), a delta-2 receptor agonist, or DPDPE, a delta-1 receptor agonist, produced a dose-dependent increase in paw-flick latency (PFL) with an ED50 of 14.0 micrograms for DELT and 30.4 micrograms for DPDPE. DAMGO, a mu receptor agonist, also increased the PFL in a dose-dependent manner when administered intrathecally with an ED50 of 0.02 microgram. Each opioid agonist increased the PFL to values that exceeded base-line latencies determined before the injection of carrageenan. However, DELT and DPDPE increased the PFL to a greater extent than did DAMGO. Coadministration of 30 micrograms of naltrindole shifted the dose-effect line of DELT to the right by 3.5-fold and that of DPDPE to the right by 2.5-fold, consistent with its characterization as a mixed delta-1/delta-2 receptor antagonist. Coadministration of 3 micrograms of naltriben (NTB) shifted the dose-effect line of DELT to the right by 3.2-fold, whereas 10 micrograms of NTB shifted the dose-effect line of DELT at least 15-fold to the right. Neither dose of NTB antagonized the effects of DPDPE. These data are consistent with characterization of NTB as a selective delta-2 receptor antagonist. The antinociception produced by DAMGO was noncompetitively antagonized by 30 micrograms of naltrindole and it was competitively antagonized by 10 micrograms of NTB. Thus, although NTB distinguishes between delta-1 and delta-2 opioid receptors, high doses may not effectively distinguish between delta and mu receptors.(ABSTRACT TRUNCATED AT 250 WORDS)