A high affinity, highly selective ligand for the delta opioid receptor: [3H]-[D-Pen2, pCl-Phe4, d-Pen5]enkephalin.
A high affinity, highly selective ligand for the delta opioid receptor: [3H]-[D-Pen2, pCl-Phe4, d-Pen5]enkephalin.
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δ 阿片受体的高亲和力、高选择性配体：[3H]-[D-Pen2、pCl-Phe4、d-Pen5]脑啡肽。
DOI：
10.1016/0024-3205(89)90154-9
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发表时间：
1989
期刊：
影响因子：
6.1
通讯作者：
Yamamura,HI
中科院分区：
文献类型：
--
作者：
Vaughn,LK;Knapp,RJ;Toth,G;Wan,YP;Hruby,VJ;Yamamura,HI
用大鼠脑匀浆测定了一种新的构象受限卤代脑啡肽类似物[~ 3 H]-[D-青霉胺2，pCl-Phe 4，D-青霉胺5]脑啡肽（[~ 3 H]pCl-DPDPE）的结合特性。在25°C下的饱和结合研究确定解离常数（Kd）为328 ± 27 pM，受体密度（Bmax）为87.2 ± 4.2 fmol/mg蛋白。动力学研究表明，[3 H]pCl-DPDPE的结合是双相的，结合速率常数分别为5.05 × 108± 2.5 × 108和0.147 ± 108± 0.014 × 108 M − 1 min −1。解离是双相的，解离速率常数为2.96 × 10−3± 0.25 × 10− 1 min −1。通过这些动力学研究测定的平均Kd值为8.4 ± 2.7 pM和201 ± 4 pM。竞争性抑制实验表明，[~ 3 H]pCl-DPDPE对δ阿片受体具有良好的选择性。相对于mu和kappa位点选择性配体所需的浓度，δ阿片受体选择性配体的低浓度可抑制[3 H]pCl-DPDPE结合。这些数据表明，[3 H]pCl-DPDPE是一种高选择性，高亲和力的配体，这应该是有用的，在表征δ阿片受体。
Binding characteristics of a new, conformationally constrained, halogenated enkephalin analogue, [3H]-[D-penicillamine2, pCl-Phe4, D-penicillamine5]enkephalin ([3H]pCl-DPDPE), were determined using homogenized rat brain tissue. Saturation binding studies at 25°C determined a dissociation constant (Kd) of 328 ± 27 pM and a receptor density (Bmax) of 87.2 ± 4.2 fmol/mg protein. Kinetic studies demonstrated biphasic association for [3H]pCl-DPDPE, with association rate constants of 5.05 × 108± 2.5 × 108and 0.147 ± 108± 0.014 × 108M−1min−1. Dissociation was monophasic with a dissociation rate constant of 2.96 × 10−3± 0.25 × 10−1min−1. The average Kdvalues determined by these kinetic studies were 8.4 ± 2.7 pM and 201 ± 4 pM. Competitive inhibition studies demonstrated that [3H]pCl-DPDPE has excellent selectively for the delta opioid receptor. [3H]pCl-DPDPE binding was inhibited by low concentrations of ligands selective for delta opioid receptor relative to the concentrations required by ligands selective for mu and kappa sites. These data show that [3H]pCl-DPDPE is a highly selective, high affinity ligand which should be useful in characterizing the delta opioid receptor.