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Interaction of antiestrogens with binding sites for muscarinic cholinergic drugs and calcium channel blockers in cell membranes.

作者信息

Batra S

机构信息

Department of Obstetrics and Gynecology, University Hospital, Lund, Sweden.

出版信息

Cancer Chemother Pharmacol. 1990;26(4):310-2. doi: 10.1007/BF02897237.

DOI:10.1007/BF02897237
PMID:2369797
Abstract

The interaction of tamoxifen and clomifene with membrane binding sites for the cholinergic ligand quinuclidinyl benzilate (QNB) and the dihydropyridine calcium antagonist nitrendipine was studied. Both tamoxifen and clomifene competed with [3H]-QNB and [3H]-nitrendipine for their binding to the receptor in the membrane fractions from the urinary bladder and myometrium. The extent of inhibition as judged by the Ki values for both antiestrogens was similar at both receptor sites. The data suggest that the antiproliferative effects of tamoxifen may involve not only the intracellular estrogen-receptor system but also receptors for neurotransmitters and membrane calcium channels.

摘要

相似文献

1
Interaction of antiestrogens with binding sites for muscarinic cholinergic drugs and calcium channel blockers in cell membranes.
Cancer Chemother Pharmacol. 1990;26(4):310-2. doi: 10.1007/BF02897237.
2
Identification and characterization of muscarinic cholinergic receptors in the isolated plasma membranes and intact tissue of the urinary bladder.膀胱分离质膜和完整组织中毒蕈碱型胆碱能受体的鉴定与特性研究
J Recept Res. 1986;6(3-4):227-46.
3
Interaction of phenoxybenzamine with muscarinic receptors and calcium channels.
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4
Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors.二氢吡啶类钙通道阻滞药对大鼠脑毒蕈碱受体和α-肾上腺素能受体的影响。
Biochem Pharmacol. 1985 Jan 15;34(2):175-80. doi: 10.1016/0006-2952(85)90121-2.
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Heterogeneity of binding sites on cardiac muscarinic receptors induced by the neuromuscular blocking agents gallamine and pancuronium.神经肌肉阻滞剂加拉明和泮库溴铵诱导的心肌毒蕈碱受体结合位点的异质性。
Mol Pharmacol. 1983 Jul;24(1):15-22.
6
Use of 3H-QNB in the isolation of plasma membrane from smooth muscle of the urinary bladder: effect of oxalate on calcium uptake by the membrane fractions.
Experientia. 1986 Jun 15;42(6):608-11. doi: 10.1007/BF01955556.
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Muscarinic cholinergic receptor subtypes in human peripheral blood lymphocytes.人类外周血淋巴细胞中的毒蕈碱型胆碱能受体亚型
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Influence of chronic oestrogen treatment on the density of muscarinic cholinergic receptors and calcium channels in the rabbit uterus.慢性雌激素治疗对兔子宫毒蕈碱型胆碱能受体和钙通道密度的影响。
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Muscarinic cholinoceptors in the rabbit's myometrium: a study of the relationship between binding and response.兔子宫肌层中的毒蕈碱型胆碱能受体：结合与反应之间关系的研究
Eur J Pharmacol. 1984 May 18;101(1-2):1-10. doi: 10.1016/0014-2999(84)90024-4.
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Tamoxifen inhibits acidification in cells independent of the estrogen receptor.

本文引用的文献

1
Antiproliferative actions of tamoxifen to human ovarian carcinomas in vitro.
Cancer Res. 1984 Jun;44(6):2265-71.
2
Microsomal binding sites for nonsteroidal anti-estrogens in MCF 7 human mammary carcinoma cells. Demonstration of high affinity and narrow specificity for basic ether derivatives of triphenylethylene.MCF 7人乳腺癌细胞中抗雌激素非甾体类药物的微粒体结合位点。三苯乙烯碱性醚衍生物具有高亲和力和特异性。
J Biol Chem. 1984 Apr 10;259(7):4223-9.
3
Calcium channel blockers: potential antimetastatic agents.钙通道阻滞剂：潜在的抗转移药物。
他莫昔芬可在不依赖雌激素受体的情况下抑制细胞酸化。
Proc Natl Acad Sci U S A. 1999 Apr 13;96(8):4432-7. doi: 10.1073/pnas.96.8.4432.
Proc Soc Exp Biol Med. 1983 Oct;174(1):16-9. doi: 10.3181/00379727-174-1-rc2.
4
Biochemical pharmacology of antiestrogen action.抗雌激素作用的生化药理学
Pharmacol Rev. 1984 Dec;36(4):245-76.
5
A comparison of two doses of tamoxifen (Nolvadex) in postmenopausal women with advanced breast cancer: 10 mg bd versus 20 mg bd.两种剂量他莫昔芬（诺瓦得士）治疗绝经后晚期乳腺癌女性的比较：每日两次，每次10毫克与每日两次，每次20毫克。
Br J Cancer. 1984 Aug;50(2):199-205. doi: 10.1038/bjc.1984.163.
6
Tamoxifen is a calmodulin antagonist in the activation of cAMP phosphodiesterase.他莫昔芬在激活环磷酸腺苷磷酸二酯酶过程中是一种钙调蛋白拮抗剂。
Biochem Biophys Res Commun. 1984 Jan 13;118(1):27-32. doi: 10.1016/0006-291x(84)91062-3.
7
Calcium: calmodulin and cancer.钙：钙调蛋白与癌症。
Fed Proc. 1982 May;41(7):2289-91.
8
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.抑制常数（K1）与导致酶促反应50%抑制率（I50）的抑制剂浓度之间的关系。
Biochem Pharmacol. 1973 Dec 1;22(23):3099-108. doi: 10.1016/0006-2952(73)90196-2.
9
Evidence that tamoxifen is a histamine antagonist.他莫昔芬是一种组胺拮抗剂的证据。
Biochem Biophys Res Commun. 1985 Sep 16;131(2):750-5. doi: 10.1016/0006-291x(85)91302-6.
10
The anti-oestrogen tamoxifen is a calcium antagonist in perfused rat mesentery.抗雌激素他莫昔芬在灌注的大鼠肠系膜中是一种钙拮抗剂。
Cancer Chemother Pharmacol. 1987;20(2):125-7. doi: 10.1007/BF00253965.