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首页> 外文期刊>Life sciences >LONG-TERM SENSITIZATION TO THE BEHAVIORAL EFFECTS OF NALTREXONE IS ASSOCIATED WITH REGIONALLY SPECIFIC CHANGES IN THE NUMBER OF MU AND DELTA OPIOID RECEPTORS IN RAT BRAIN
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LONG-TERM SENSITIZATION TO THE BEHAVIORAL EFFECTS OF NALTREXONE IS ASSOCIATED WITH REGIONALLY SPECIFIC CHANGES IN THE NUMBER OF MU AND DELTA OPIOID RECEPTORS IN RAT BRAIN

机译：对纳曲酮行为影响的长期敏感性与大鼠脑中MU和δ阿片样物质受体数量的区域特定变化有关

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Enhanced sensitivity to some of the behavioral effects of the opioid antagonist naltrexone (NTX) develops following once-weekly injections of cumulative doses of the drug. Rats treated with this regimen of NTX injections show enhanced sensitivity to the operant response rate decreasing effects of NTX and NTX-induced salivation. The enhanced sensitivity is long-lasting and appears to be produced through conditioning processes. We have conducted saturation binding assays to assess possible changes in the number and affinity of mu and delta opioid receptors in cortical, midbrain and hindbrain membrane preparations from Long-Evans rats treated once weekly for 8 weeks with cumulative doses of the drug (1, 3, 10, 30 and 100 mg/kg). H-3-DAMGO (0.5-21 nM) and H-3-pCl-DPDPE (0.04-4 nM) were used to characterize mu and delta receptors, respectively. NTX treatment had no effect on H-3-DAMGO binding in cortex, but decreased binding in midbrain and increased binding in hindbrain relative to saline-treated controls. Saturation analyses revealed that these differences reflected changes in the number, but not the affinity of mu receptors. NTX treatment also increased the amount of H-3-pCl-DPDPE bound to delta receptors in midbrain and hindbrain, but not in cortex. Again, these changes were due to changes in the number of receptors. Thus, chronic NTX differentially affects the number of mu and delta opioid receptors in various brain regions. [References: 16]
机译：每周一次注射累积剂量的药物后，对阿片类药物拮抗剂纳曲酮（NTX）的某些行为影响的敏感性增强。用这种NTX注射方案治疗的大鼠对NTX和NTX诱导的唾液分泌的手术反应率降低作用显示出更高的敏感性。增强的灵敏度是持久的，并且似乎是通过调节过程产生的。我们进行了饱和结合测定，以评估长期服用每周8周，用累积剂量的药物治疗的Long-Evans大鼠的皮质，中脑和后脑膜制剂中mu和delta阿片受体的数量和亲和力的可能变化（1、3 ，10、30和100 mg / kg）。使用H-3-DAMGO（0.5-21 nM）和H-3-pCl-DPDPE（0.04-4 nM）分别表征mu和delta受体。 NTX处理对皮层中H-3-DAMGO的结合没有影响，但是相对于盐水处理的对照，中脑的结合减少，后脑的结合增加。饱和度分析表明，这些差异反映的是数量变化，而不反映mu受体的亲和力。 NTX处理还增加了与中脑和后脑的δ受体结合的H-3-pCl-DPDPE的量，但在皮质中没有。同样，这些变化是由于受体数目的变化。因此，慢性NTX差异性地影响各个脑区的μ和δ阿片受体的数量。 [参考：16]

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