SELECTIVITY OF LIGAND-BINDING TO OPIOID RECEPTORS IN BRAIN MEMBRANES FROM THE RAT, MONKEY AND GUINEA-PIG
SELECTIVITY OF LIGAND-BINDING TO OPIOID RECEPTORS IN BRAIN MEMBRANES FROM THE RAT, MONKEY AND GUINEA-PIG
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DOI：
10.1016/0014-2999(88)90112-4
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发表时间：
1988-04-13
影响因子：
5
通讯作者：
MEDZIHRADSKY, F
中科院分区：
文献类型：
--
作者：
CLARK, MJ;CARTER, BD;MEDZIHRADSKY, F
[~3H]舒芬太尼与阿片受体平衡结合条件选择性)，[~3H][D-Pen2，D-Pen5]脑啡肽(选择性)和[~3H]U69,593(.kappa.选择性)建立在大鼠大脑、货币皮质或豚鼠小脑的细胞膜上。各种阿片类生物碱和多肽与单位、β或卡帕结合的选择性指数。阿片受体被表示为取代两个选择性放射性标记配体的EC50值的比率：[~3H]舒芬太尼/[~3H](D-Pen2，D-Pen5)脑啡肽(选择性：单位/单位)，[~3H]舒芬太尼/[~3H]U69,593(选择性：单位/kappa)，或[~3H][D-Pen2，D-Pen5]脑啡肽/[~3H]U69.593(选择性：单位/单位)。观察到结合选择性的高分辨率：在大鼠脑中。TYR-D-ALA-Gly-(Me)Phe-Gly-ol和舒芬太尼的选择性为0.02和0.03，而[D-Pen2，D-Pen5]脑啡肽和ICI 174,864的选择性为1200和998。与.MU相比。阿片类药物，Delta.的特定结合。还有.卡帕。激动剂对钠的敏感性较低。这些结果描述了一种常规适用的方法学方法，用于评估选择性配体与单位、三角洲的结合。还有.卡帕。啮齿动物和猴子脑膜上的阿片受体。
Conditions for the equilibrium binding to opioid receptor of [3H](sufentanil (.mu. selective), [3H][D-Pen2,D-Pen5]enkephalin (.delta. selective), and [3H]U69,593 (.kappa. selective) were established in membranes from rat brain cerebrum, money cortex, or guinea pig cerebellum. The selectivity index of various opioid alkaloids and peptides in binding to the .mu., .delta., or .kappa. opioid receptors was expressed as the ratio of the EC50 values in displacing two selective radiolabeled ligands: [3H]sufentanil/[3H](D-Pen2,D-Pen5)enkephalin (selectivity: .mu./.delta.), [3H]sufentanil/[3H]U69,593 (selectivity: .mu./.kappa.), or [3H][D-Pen2,D-Pen5]enkephalin/[3H]U69.593 (selectivity: .delta./.kappa.). High resolution in binding selectivity was observed: in rat brain the .mu./.delta. selectivity for Tyr-D-Ala-Gly-(Me)Phe-Gly-ol and sufentanil were 0.02 and 0.03, whereas for [D-Pen2,D-Pen5]enkephalin and ICI 174,864 they were 1200 and 998. Compared to .mu. opiates, the specific binding of .delta. and .kappa. agonists was less sensitive to sodium. The results describe a routinely applicable methodological approach for the assessment of selective ligand binding to the .mu., .delta. and .kappa. opioid receptors in rodent and monkey brain membranes.