巴比妥酸盐结合烟碱乙酰胆碱receptor-rich膜的变构管理网站。

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Dodson BA、科布市LM米勒千瓦

巴比妥酸盐结合烟碱乙酰胆碱receptor-rich膜的变构管理网站。

摩尔杂志。1987年7月,32(1):119 - 26所示。

PubMed ID

3600612 (在PubMed

]

文摘

巴比妥酸盐与乙酰胆碱的能力receptor-rich膜纯化的electroplaques鱼雷nobiliana被离心试验检查。[14 c]异戊巴比妥分区成膜和可替换的绑定到一个网站和一个平衡12 microM的离解常数。这种低亲和力的化学计量学很难获得,尽管高特定活动的乙酰胆碱受体膜制备。然而,数据不符合化学计量学每acetylcholine-binding barbiturate-binding一个网站的网站。可替换的[14 c]异戊巴比妥绑定是完全被巴比妥酸盐(IC50:异戊巴比妥、28 microM;司可巴比妥,110 microM;戊巴比妥,400 microM;苯巴比妥,690 microM;690年butabarbital microM;和巴比妥,5.1 mM. alpha-Bungarotoxin没有影响,但是胆碱能配体,将乙酰胆碱受体麻木的状态(乙酰胆碱,carbamylcholine,在较小程度上,d-tubocurarine)部分抑制可替换的[14 c]异戊巴比妥绑定。 This cholinergic inhibition was prevented by preincubation with alpha-bungarotoxin, implying an allosteric mediation through the classical cholinergic site. This negative interaction between the cholinergic and the barbiturate sites was mutual with barbiturates partially decreasing equilibrium [3H]acetylcholine binding in a saturable fashion with relative affinities that parallel those for inhibiting [14C]amobarbital binding (IC50). These data establish a mutual negative heterotropic interaction between barbiturate-binding sites and cholinergic binding sites on the nicotinic acetylcholine receptor from Torpedo.

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药物

Butabarbital