[3H] -前列环素与神经体细胞杂种膜的结合。
The binding of [3H]-prostacyclin to membranes of a neuronal somatic hybrid.
作者信息
Blair I A, MacDermot J
出版信息
Br J Pharmacol. 1981 Mar;72(3):435-41. doi: 10.1111/j.1476-5381.1981.tb10994.x.
Abstract
1 [3H]-prostacyclin bound to a washed membrane preparation of the NCB-20 neuronal hybrid cell line. 2 Kinetic analysis of [3H]-prostacyclin binding suggested a simple, non-cooperative bimolecular interaction between the ligand and a single receptor population. The equilibrium dissociation constant was 16.6 nM, and binding at a saturating [3H]-prostacyclin concentration enabled the receptor density of 2.57 x 10(5) receptor molecules per cell to be calculated. 3 At 20 degrees C the rate constant for the forward reaction (K+1) was 2.26 x 10(5) M-1 S-1, and the rate constant for the dissociation of the ligand-receptor complex (k-1) was 3.85 x 10(-3) S-1. Thus the dissociation constant (k-1/k+1) was 17.0 nM. 4 Prostaglandin E1 and prostacyclin compete for a single receptor in these cells, and comparison of other prostaglandins as inhibitors of [3H]-prostacyclin binding revealed some of the structural requirements for high-affinity occupation of prostacyclin receptors.
摘要
- [3H] - 前列环素与NCB - 20神经杂交细胞系的洗涤后膜制剂结合。2. [3H] - 前列环素结合的动力学分析表明，配体与单一受体群体之间存在简单的、非协同的双分子相互作用。平衡解离常数为16.6 nM，在饱和[3H] - 前列环素浓度下的结合使得能够计算出每个细胞2.57×10(5)个受体分子的受体密度。3. 在20℃时，正向反应的速率常数（K+1）为2.26×10(5) M-1 S-1，配体 - 受体复合物解离的速率常数（k-1）为3.85×10(-3) S-1。因此，解离常数（k-1/k+1）为17.0 nM。4. 前列腺素E1和前列环素在这些细胞中竞争单一受体，并且将其他前列腺素作为[3H] - 前列环素结合抑制剂进行比较，揭示了前列环素受体高亲和力占据的一些结构要求。
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