2℃和37℃时一系列作用于豚鼠海马体苯二氮䓬受体的配体的抑制常数和GABA位移。

Inhibition constants and GABA-shifts at 2 degrees C and 37 degrees C for a spectrum of ligands acting on the benzodiazepine receptors of guinea pig hippocampus.

Dawson R M, Poretski M

Materials Research Laboratory, Defence Science and Technology Organisation, Ascot Vale, Vic, Australia.

Gen Pharmacol. 1989;20(6):843-8. doi: 10.1016/0306-3623(89)90341-8.

Abstract

Dissociation constants and Hill coefficients were determined for 13 ligands inhibiting the binding of [3H]flunitrazepam to the benzodiazepine receptors of guinea pig hippocampus at 2 degrees C and 37 degrees C. 2. The ratio of I50 in the absence of gamma-aminobutyric acid (GABA) to that in the presence of 10(-5) M GABA (the GABA-shift) was found to vary from 0.4 to 2.5. 3. There was no correlation between the pharmacological activity of the ligand and the GABA-shift, or between the pharmacological activity and the magnitude of the increase in affinity of the ligand for the receptor as the temperature decreased from 37 degrees C to 2 degrees C. 4. A correlation was observed between the temperature-induced affinity change and the GABA-shift at 37 degrees C.

摘要

测定了13种配体在2℃和37℃时抑制[3H]氟硝西泮与豚鼠海马体苯二氮䓬受体结合的解离常数和希尔系数。2. 发现不存在γ-氨基丁酸（GABA）时的I50与存在10^(-5) M GABA时的I50之比（GABA位移）在0.4至2.5之间变化。3. 配体的药理活性与GABA位移之间，以及药理活性与温度从37℃降至2℃时配体对受体亲和力增加的幅度之间均无相关性。4. 在37℃时观察到温度诱导的亲和力变化与GABA位移之间存在相关性。