Inhibitory effects of NaCl and guanyl-5'yl-imidodiphosphate (GppNHp) on [3H]naloxone binding to kappa-opioid receptors in guinea pig cerebellum.
Inhibitory effects of NaCl and guanyl-5'yl-imidodiphosphate (GppNHp) on [3H]naloxone binding to kappa-opioid receptors in guinea pig cerebellum.
复制标题
NaCl 和鸟苷基-5基-亚胺二磷酸 (GppNHp) 对[3H]纳洛酮与豚鼠小脑中 kappa-阿片受体结合的抑制作用。
DOI：
10.1248/bpb.16.921
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发表时间：
1993
影响因子：
2
通讯作者：
Y. Murakoshi
中科院分区：
文献类型：
--
作者：
K. Ishige;M. Makimura;Y. Ito;Y. Murakoshi
用放射性标记的阿片受体拮抗剂[~3H]纳洛酮、[~3H]丙诺啡和Kappa激动剂[~3H]U-69593对豚鼠脑内阿片受体进行了研究。氯化钠、5‘-鸟氨基-二磷酸鸟苷(GppNHp)和氯化钠+GppNHp降低了[~3H]U-69593与豚鼠小脑膜的结合，氯化钠和GppNHp也降低了[~3H]纳洛酮与小脑膜的结合。在豚鼠大脑皮层、纹状体和大鼠小脑，GppNHp在存在或不存在100 nM[D-Ala2，N-Me-Phe4，Gly5-ol]脑啡肽(DAMGO)和[D-Ala2，D-Leu5]脑啡肽(DADLE)的情况下，对[~3H]纳洛酮结合无明显影响。氯化钠、GppNHp或氯化钠+GppNHp对豚鼠小脑[~3H]丙诺啡结合无明显影响。此外，N-乙基马来酰亚胺(NEM)预处理小脑膜后，[~3H]纳洛酮结合减少，这也减弱了GppNHp对小脑[~3H]纳洛酮结合的抑制作用。这些结果表明，豚鼠小脑与[~H]纳洛酮的结合特性不同于其他脑区和大鼠小脑，[~~H]纳洛酮和[~3H]U-69593与豚鼠小脑阿片受体的相互作用与G蛋白有关，而与[~H]异丙诺啡无关。
Studies were performed to characterize the opioid receptors in guinea pig brain using the radiolabeled opioid antagonists, [3H]naloxone and [3H]diprenorphine and the kappa-agonist [3H]U-69593. The binding of [3H]U-69593 to guinea pig cerebellar membranes was reduced by NaCl, guanyl-5'yl-imidodiphosphate (GppNHp) and NaCl+GppNHp, and [3H]naloxone binding to cerebellar membranes was also reduced by NaCl and GppNHp. In the guinea pig cerebral cortex and striatum and the rat cerebellum, [3H]naloxone binding was not affected significantly by GppNHp in the presence or absence of 100 nM [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAMGO) and [D-Ala2, D-Leu5]enkephalin (DADLE). Guinea pig cerebellar [3H]diprenorphine binding was not affected by NaCl, GppNHp or NaCl+GppNHp. Furthermore, [3H]naloxone binding was reduced after pretreating cerebellar membranes with N-ethylmaleimide (NEM), which also attenuated GppNHp-induced inhibition of cerebellar [3H]naloxone binding. These results suggest that the properties of [3H]naloxone binding in guinea pig cerebellum differ from those in other brain regions and rat cerebellum, and that the interaction of [3H]naloxone and [3H]U-69593, but not [3H]diprenorphine, with guinea pig cerebellar opioid receptors is associated with a G-protein.