The binding sites of the calcium antagonist [3H] PN 200110 in the human myometrium and myosalpinx
The binding sites of the calcium antagonist [3H] PN 200110 in the human myometrium and myosalpinx
复制标题
钙拮抗剂 [3H] PN 200110 在人子宫肌层和输卵管肌中的结合位点
DOI：
10.3109/00016348609157029
复制
发表时间：
1986
影响因子：
4.3
通讯作者：
Anne Weidacher
中科院分区：
文献类型：
--
作者：
Jürgen Kleinstein;Peter Betjemann;Anne Weidacher
二氢吡啶类钙拮抗剂由于其抑制子宫收缩的能力，可能被证明是治疗早产的重要辅助药物。在45000 × g人子宫肌层和输卵管肌层膜制备物中集中了钙受体阻滞剂的特异性结合位点。[3 H] PN 200110（一种苯并恶二唑取代的二氢吡啶衍生物）结合的Scatchard图分析显示，子宫肌层膜的结合位点数在500 - 700 fmol/mg蛋白（Bmax）之间，亲和力（KD）为0.3±0.1 nmol/1。在肌输卵管膜制备物中，Bmax在250和300 fmol/mg蛋白质之间，KD值为0.9±0.1 nmol/l。未标记的钙拮抗剂取代[3 H] PN 200110结合，效价排序如下：尼群地平±硝苯地平±d-西地尔硫卓>D-600±硫帕米。在子宫背壁的肌层中，钙通道特别密集（796±186 fmoles/mg蛋白）。输卵管肌中结合位点的数量在峡部最多（242±23 fmoles/mg蛋白）。
Calcium antagonists of the dihydropyridine type may prove to be an important adjunct to the therapy of premature labor due to their proven ability to inhibit uterine contractility. Specific binding sites for calcium blockers were concentrated in 45 000 × g membrane preparations of human myometrium and myosalpinx. Scatchard plot analysis of the binding of [3H] PN 200110, a benzoxadiazole‐substituted dihydropyridine derivate, revealed that the binding sites of myometrial membranes numbered between 500 and 700 fmoles/mg protein (Bmax) and had an affinity (KD) of 0.3±0.1 nmol/1. In myosalpingeal membrane preparations Bmax was between 250 and 300 fmoles/mg protein, with KD values of 0.9±0.1 nmol/1. Unlabelled calcium anta‐gonits displaced [3H] PN 200110 binding in the following order of potency ranking: nitrendipine±nifedipine±d‐cisdiltiazem >D‐600±tiapamil. The calcium channels were especially dense (796±186 fmoles/mg protein) in the myometrium of the dorsal uterine wall. The number of binding sites in the myosalpinx was greatest in the isthmus (242±23 fmoles/mg protein).
Ca 通道拮抗剂 [3H]尼群地平与豚鼠回肠平滑肌结合的表征。
DOI：
--
发表时间：
1983
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Bolger,GT;Gengo,P;Klockowski,R;Luchowski,E;Siegel,H;Janis,RA;Triggle,AM;Triggle,DJ
通讯作者：
Triggle,DJ