Differential cross-tolerance between analgesia produced by alpha 2-adrenoceptor agonists and receptor subtype selective opioid treatments.
Differential cross-tolerance between analgesia produced by alpha 2-adrenoceptor agonists and receptor subtype selective opioid treatments.
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α2-肾上腺素受体激动剂和受体亚型选择性阿片类药物治疗产生的镇痛之间存在差异交叉耐受性。
DOI：
10.1016/0014-2999(94)00695-4
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发表时间：
1995
影响因子：
5
通讯作者：
Tran,JG
中科院分区：
文献类型：
--
作者：
Paul,D;Tran,JG
用小鼠甩尾法研究了α_2肾上腺素能受体与阿片受体激动剂的镇痛交叉耐受性。耐受可乐定（0.3 mg/kg s.c.）的小鼠或甲苯噻嗪（7 mg/kg s.c.）对吗啡（5 mg/kg s.c.）交叉耐受，纳洛啡（70 mg/kg s.c.）和脊髓上[d-Ala 2，MePhe 4，Gly（ol）5]脑啡肽（DAMGO; 4 ng i. c. v.），但不包括反式-（±）-3，4-二氯-N-甲基-N-[2-（1-吡咯烷基）-环己基]苯乙酰胺甲磺酸盐（U 50，488; 5 mg/kg s.c.），脊髓DAMGO（10 ng i.t.），脊髓上[d-Pen 2，d-Pen 5]脑啡肽（DPDPE; 9 μg i. c. v.）或脊髓DPDPE（700 ng i.t.）。在补充研究中，对吗啡和纳洛啡耐受的小鼠对这两种α2-肾上腺素受体激动剂交叉耐受，但U 50，488耐受小鼠则不然。结果表明α2-肾上腺素受体与μ1−、μ2−、δ−、κ1−和κ3-阿片类镇痛回路之间存在差异性相互作用。
Analgesic cross-tolerance between α2-adrenoceptor and opioid receptor agonists was studied using the mouse tail-flick assay. Mice tolerant to clonidine (0.3 mg/kg s.c.) or xylazine (7 mg/kg s.c.) were cross-tolerant to morphine (5 mg/kg s.c.), nalorphine (70 mg/kg s.c.) and supraspinal [d-Ala2,MePhe4,Gly(ol)5]enkephalin (DAMGO; 4 ng i.c.v.), but not trans-(±)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl] benzeneacetamide methanesulfonate (U50,488; 5 mg/kg s.c.), spinal DAMGO (10 ng i.t.), supraspinal [d-Pen2,d-Pen5]enkephalin (DPDPE; 9 μg i.c.v.) or spinal DPDPE (700 ng i.t.). In the complimentary studies, mice tolerant to morphine and nalorphine were cross-tolerant to both of the α2-adrenoceptor agonists, but U50,488 tolerant mice were not. The results suggest differential interactions between α2-adrenoceptor and μ1−, μ2−, δ−, κ1−and κ3-opioid analgesic circuitry.