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抗雌激素他莫昔芬的钙拮抗作用。

Calcium antagonism by the antioestrogen tamoxifen.

作者信息

Lipton A, Morris I D

出版信息

Cancer Chemother Pharmacol. 1986;18(1):17-20. doi: 10.1007/BF00253056.

DOI:10.1007/BF00253056
PMID:3757153
Abstract

Tamoxifen, an oestrogen receptor antagonist and an effective treatment for breast carcinoma, has recently been shown to possess spasmolytic activity in smooth muscle. Tamoxifen in vitro inhibited the contraction of smooth muscle from rat myometrium and aorta produced by exogenous calcium. At the same concentration tamoxifen did not affect the uptake of calcium into the muscle. The importance of calcium in cell proliferation suggests that some of the unexplained antitumor activity of the oestrogen antagonists may be accounted for by intracellular calcium antagonism.

摘要

他莫昔芬是一种雌激素受体拮抗剂,也是治疗乳腺癌的有效药物,最近已被证明在平滑肌中具有解痉活性。他莫昔芬在体外可抑制外源性钙引起的大鼠子宫肌层和平滑肌的收缩。在相同浓度下,他莫昔芬不影响肌肉对钙的摄取。钙在细胞增殖中的重要性表明,雌激素拮抗剂一些无法解释的抗肿瘤活性可能是由细胞内钙拮抗作用引起的。

相似文献

1
Calcium antagonism by the antioestrogen tamoxifen.抗雌激素他莫昔芬的钙拮抗作用。
Cancer Chemother Pharmacol. 1986;18(1):17-20. doi: 10.1007/BF00253056.
2
Inhibition of intestinal smooth muscle function by tamoxifen and clomiphene.他莫昔芬与克罗米酚对肠道平滑肌功能的抑制作用。
Life Sci. 1985 Jul 22;37(3):273-8. doi: 10.1016/0024-3205(85)90653-8.
3
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.
4
The action of cinnarizine on the contraction induced by calcium in depolarized arterial and intestinal smooth muscle preparations.桂利嗪对去极化动脉和肠道平滑肌制剂中钙诱导收缩的作用。
Arch Int Pharmacodyn Ther. 1972 Jun;197(2):399-400.
5
[Antagonism between cyclic AMP and calcium on isolated depolarized aorta in the rat].[环磷酸腺苷与钙在大鼠离体去极化主动脉上的拮抗作用]
J Physiol (Paris). 1972;65:Suppl 3:387A+.
6
Acute inhibition of rat myometrial responses to oxytocin by tamoxifen stereoisomers and oestradiol.他莫昔芬立体异构体和雌二醇对大鼠子宫肌层催产素反应的急性抑制作用。
J Endocrinol. 1984 Dec;103(3):383-8. doi: 10.1677/joe.0.1030383.
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Properties of intracellular calcium stores in pregnant rat myometrium.妊娠大鼠子宫肌层细胞内钙库的特性
Br J Pharmacol. 1988 Sep;95(1):284-90. doi: 10.1111/j.1476-5381.1988.tb16575.x.
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Effects of the calcium channel facilitator, CGP 28,392, on different modes of contraction in smooth muscle of rabbit and rat aortae and guinea-pig taenia caeci.钙通道促进剂CGP 28392对兔和大鼠主动脉及豚鼠盲肠带平滑肌不同收缩模式的影响
Br J Pharmacol. 1986 Oct;89(2):423-9. doi: 10.1111/j.1476-5381.1986.tb10276.x.
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Calcium and angiotensin tachyphylaxis in rat uterine smooth muscle.大鼠子宫平滑肌中的钙与血管紧张素快速耐受性
Am J Physiol. 1975 May;228(5):1423-30. doi: 10.1152/ajplegacy.1975.228.5.1423.
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Calcium and contractions of isolated smooth muscle cells from rat myometrium.钙与大鼠子宫肌层分离的平滑肌细胞的收缩
Can J Physiol Pharmacol. 1987 Sep;65(9):1966-75. doi: 10.1139/y87-306.

引用本文的文献

1
Tamoxifen and secondary tumours. An update.他莫昔芬与继发性肿瘤。最新进展。
Drug Saf. 1997 Feb;16(2):104-17. doi: 10.2165/00002018-199716020-00003.
2
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.
3
Characterisation of a tamoxifen-resistant variant of the ZR-75-1 human breast cancer cell line (ZR-75-9a1) and ability of the resistant phenotype.ZR-75-1人乳腺癌细胞系(ZR-75-9a1)他莫昔芬耐药变体的特征及耐药表型的能力。

本文引用的文献

1
The need for calcium in the contractile responses induced by acetylcholine and potassium in the rat uterus.大鼠子宫中乙酰胆碱和钾诱导的收缩反应对钙的需求。
J Physiol. 1962 May;161(3):424-41. doi: 10.1113/jphysiol.1962.sp006897.
2
Effects of biologically active metabolites of tamoxifen on the proliferation kinetics of MCF-7 human breast cancer cells in vitro.他莫昔芬生物活性代谢产物对MCF-7人乳腺癌细胞体外增殖动力学的影响。
Cancer Res. 1983 Oct;43(10):4618-24.
3
Antitumor effect of a calmodulin antagonist on the growth of solid sarcoma-180.
Br J Cancer. 1989 Apr;59(4):522-6. doi: 10.1038/bjc.1989.107.
Cancer Lett. 1983 Jun;19(2):215-20. doi: 10.1016/0304-3835(83)90157-x.
4
Circumvention of vincristine and Adriamycin resistance in vitro and in vivo by calcium influx blockers.钙内流阻滞剂在体外和体内对长春新碱及阿霉素耐药性的规避作用
Cancer Res. 1983 Jun;43(6):2905-10.
5
Effects of estradiol and tamoxifen on human breast cancer cells in serum-free culture.雌二醇和他莫昔芬对无血清培养的人乳腺癌细胞的影响。
Cancer Res. 1984 Jul;44(7):2790-3.
6
Factors affecting the sensitivity of T-47D human breast cancer cells to tamoxifen.影响T-47D人乳腺癌细胞对他莫昔芬敏感性的因素。
Cancer Res. 1984 Jun;44(6):2398-405.
7
Estrogen receptor-mediated and cytotoxic effects of the antiestrogens tamoxifen and 4-hydroxytamoxifen.抗雌激素他莫昔芬和4-羟基他莫昔芬的雌激素受体介导作用及细胞毒性作用。
Cancer Res. 1984 Apr;44(4):1409-14.
8
Inhibition of human breast cancer colony formation by anticalmodulin agents: trifluoperazine, W-7, and W-13.抗钙调蛋白药物(三氟拉嗪、W-7和W-13)对人乳腺癌集落形成的抑制作用
Cancer Chemother Pharmacol. 1983;11(2):86-90. doi: 10.1007/BF00254251.
9
Acute inhibition of rat myometrial responses to oxytocin by tamoxifen stereoisomers and oestradiol.他莫昔芬立体异构体和雌二醇对大鼠子宫肌层催产素反应的急性抑制作用。
J Endocrinol. 1984 Dec;103(3):383-8. doi: 10.1677/joe.0.1030383.
10
The pharmacology and clinical uses of tamoxifen.他莫昔芬的药理学及临床应用。
Pharmacol Ther. 1984;25(2):127-205. doi: 10.1016/0163-7258(84)90043-3.