乙二胺类似物和衍生物对苯二氮䓬受体结合增强作用的构效关系研究
Structure-activity studies on the potentiation of benzodiazepine receptor binding by ethylenediamine analogues and derivatives.
作者信息
Morgan P F, Stone T W
出版信息
Br J Pharmacol. 1983 Aug;79(4):973-7. doi: 10.1111/j.1476-5381.1983.tb10543.x.
The effect of ethylenediamine analogues on in vitro binding of [3H]-diazepam to crude cerebral cortical synaptosomal membranes in the rat was studied. Ethylenediamine significantly increased [3H]-diazepam binding to a maximum potentiation of 154% control (EC50 = 1.8 X 10(-4) M) and was the most active compound studied in terms of both potency and the maximum potentiation observed. Potentiation of [3H]-diazepam binding by ethylenediamine analogues is dependent on carbon-chain length, appears to require two terminal amino groups, and is not observed in the rigid analogues studied. Potentiation of [3H]-diazepam binding by ethylenediamine analogues is mediated largely by a change in receptor number and not receptor affinity. Results are discussed in terms of the possible nature of the ethylenediamine binding site.
研究了乙二胺类似物对大鼠大脑皮层粗制突触体膜上[³H] - 地西泮体外结合的影响。乙二胺显著增加[³H] - 地西泮的结合，最大增强至对照的154%（半数有效浓度 = 1.8×10⁻⁴ M），并且就效力和观察到的最大增强而言，是所研究的最具活性的化合物。乙二胺类似物对[³H] - 地西泮结合的增强取决于碳链长度，似乎需要两个末端氨基，在所研究的刚性类似物中未观察到这种增强。乙二胺类似物对[³H] - 地西泮结合的增强主要由受体数量的变化而非受体亲和力介导。根据乙二胺结合位点的可能性质对结果进行了讨论。
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