Interaction of Opiates with Opioid Binding Sites in the Bovine Adrenal Medulla: I. Interaction with δ and μ Sites
Interaction of Opiates with Opioid Binding Sites in the Bovine Adrenal Medulla: I. Interaction with δ and μ Sites
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阿片类药物与牛肾上腺髓质中阿片类药物结合位点的相互作用：I. 与 δ 和 μ 位点的相互作用
DOI：
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发表时间：
1985
期刊：
影响因子：
--
通讯作者：
C. Oliver
中科院分区：
文献类型：
--
作者：
E. Castanas;N. Bourhim;P. Giraud;F. Boudouresque;P. Cantau;C. Oliver
翻译后摘要：在本研究中，我们研究了阿片类药物与牛肾上腺髓质中的δ和μ阿片类药物结合位点的相互作用。在饱和浓度的吗啡肽存在下的[3 H][D-Ala 2，D-Leu 5]-脑啡肽（[3 H]DADLE）用于分析δ位点相互作用，而在饱和浓度的[D-Ser 2，Leu 5]-脑啡肽Thr 6（DSLET）或[3 H][D-Ala 2，Me-Phe 4，Gly 5-ol]-脑啡肽（[3 H]DAGO）存在下的[3 H]DADLE用于测定μ位点。这两个结合位点被发现与阿片类药物立体选择性相互作用。蛋白水解酶（胰蛋白酶、α-糜蛋白酶、胃蛋白酶）、N-乙基马来酰亚胺和A2-磷脂酶对结合的影响不同。动力学和平衡结合研究表明，在每种情况下，放射性标记的阿片类药物与一类结合位点相互作用，遵循简单的二级双分子动力学。阿片类药物和阿片肽对结合的竞争证实了这些位点的δ和μ选择性。一价（Na+，Li+，K+）和二价（Mg 2+，Mn 2+，Ca 2+）离子与这两个结合位点的相互作用差异：在一般情况下，一价阳离子优先影响结合位点的表观数量，而二价离子修改的平衡解离常数。此外，在某些离子条件下，检测到的结合位点的正或负的协同性和明显的异质性。
Abstract: In the present study we examined the interaction of opiates with the δ and μ opioid binding sites in the bovine adrenal medulla. [3H][D‐Ala2, D‐Leu5]‐enkephalin ([3H]DADLE) in the presence of saturating concentrations of morphiceptin was used to analyze δ site interactions, whereas either [3H]DADLE in the presence of saturating concentrations of [D‐Ser2, Leu5]‐enkephalinThr6 (DSLET) or [3H][D‐Ala2, Me‐Phe4, Gly5‐ol]‐enkephalin ([3H]DAGO) was used for the determination of μ sites. Both binding sites were found to interact stereo selectively with opiates. The binding was affected differentially by proteolytic enzymes (trypsin, α‐chymotrypsin, pepsin), N‐ethylmaleimide, and A2‐phospholipase. Kinetic and equilibrium binding studies revealed that in each case radiolabeled opiates interact with one class of binding sites, following simple second‐order bi molecular kinetics. Competition for binding by opiates and opioid peptides confirmed the δ and μ selectivity of these sites. Monovalent (Na+, Li+, K+) and divalent (Mg2+, Mn2+, Ca2+) ions interacted differentially with these two binding sites: In general, monovalent cations affected preferentially the apparent number of binding sites, whereas divalent ions modified the equilibrium dissociation constant. Furthermore, positive or negative cooperativity and an apparent heterogeneity of binding sites were detected under some ionic conditions.
影响因子：
3.6
作者：
P. Law;D. Hom;H. Loh
通讯作者：
P. Law;D. Hom;H. Loh
药物-受体相互作用的定量分析：I.动力学和平衡特性的测定。
影响因子：
6.1
作者：
Weiland,GA;Molinoff,PB
通讯作者：
Molinoff,PB
β-内啡肽：兔小脑和脑膜结合位点的特征。
DOI：
10.1016/0006-291x(83)91412-2
发表时间：
1983
影响因子：
3.1
作者：
Ho,CL;HammondsJr,RG;Li,CH
通讯作者：
Li,CH