LONG-TERM SENSITIZATION TO THE ACTIVATION OF CEREBRAL DELTA-OPIOID RECEPTORS BY THE DELTORPHIN TYR-D-ALA-PHE-GLU-VAL-VAL-GLY-NH2 IN RATS EXPOSED TO MORPHINE
LONG-TERM SENSITIZATION TO THE ACTIVATION OF CEREBRAL DELTA-OPIOID RECEPTORS BY THE DELTORPHIN TYR-D-ALA-PHE-GLU-VAL-VAL-GLY-NH2 IN RATS EXPOSED TO MORPHINE
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DOI：
10.1073/pnas.89.9.3696
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发表时间：
1992-05-01
影响因子：
11.1
通讯作者：
ERSPAMER, V
中科院分区：
文献类型：
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作者：
MELCHIORRI, P;MARITATI, M;ERSPAMER, V
在评估脑内阿片受体激活的反应的实验中，每天重复向大鼠脑内注射选择性的阿片受体激动剂Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2([D-Ala2]Deltorphin II)可使大鼠产生耐受，而每日重复注射或持续注射吗啡可使大鼠对阿片受体激动剂的行为激活效应增敏。尽管大鼠在吗啡戒断后没有改变其自发的运动活动，但它们对三角洲阿片激动剂的挑战剂量的运动和刻板印象产生的影响变得明显的高反应。在停止吗啡治疗后，对增量阿片受体激活的敏感化至少持续了60天。这些结果表明，对阿片类药物的耐受性和长期敏感化的发展涉及到阿片受体。
In experiments to evaluate responses to the activation of cerebral delta-opioid receptors, repeated daily injection of the selective delta-opioid agonist Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 ([D-Ala2]deltorphin II) into rat brain resulted in the development of tolerance, whereas repeated daily injection or continuous infusion of morphine resulted in sensitization to the behavioral activating effects of the delta-opioid agonist. Although the rats did not modify their spontaneous locomotor activity after morphine withdrawal, they became markedly hyperresponsive to the locomotor and stereotypy-producing effects of a challenge dose of the delta-opioid agonist. Sensitization to activation of delta-opioid receptors persisted for at least 60 days after discontinuing morphine treatment. These results show that the development of tolerance and long-term sensitization to opioids involves delta-opioid as well as mu-opioid receptors.