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外周型苯二氮䓬受体配体抗增殖作用的一个新方面。

A new aspect of the antiproliferative action of peripheral-type benzodiazepine receptor ligands.

作者信息

Camins A, Diez-Fernandez C, Pujadas E, Camarasa J, Escubedo E

机构信息

Unidad de Farmacología y Farmacognosia, Universidad de Barcelona, Facultad de Farmacia, Zona Universidad Pedralbes, Barcelona, Spain.

出版信息

Eur J Pharmacol. 1995 Jan 16;272(2-3):289-92. doi: 10.1016/0014-2999(94)00652-n.

DOI:10.1016/0014-2999(94)00652-n
PMID:7713173
Abstract

Ro 5-4864 (4-chlorodiazepam), PK 11195 (1-(2-chlorophenyl)-1,3-dihydro-1-methyl-propyl)isoquinoline carboxamide) and diazepam inhibit, in a concentration-dependent way, the proliferation of V79 Chinese hamster lung cells (IC50 values were: 65.0 +/- 3.73 microM, 57.70 +/- 4.75 microM and 106.80 +/- 8.89 microM, respectively) without being cytotoxic. This antiproliferative effect is mediated by mitosis arrest in the G2 + M stage without affecting DNA synthesis and seems unrelated to a specific interaction of these drugs with the peripheral-type benzodiazepine receptor.

摘要

Ro 5-4864(4-氯地西泮)、PK 11195(1-(2-氯苯基)-1,3-二氢-1-甲基丙基)异喹啉甲酰胺)和地西泮以浓度依赖性方式抑制V79中国仓鼠肺细胞的增殖(IC50值分别为:65.0±3.73微摩尔、57.70±4.75微摩尔和106.80±8.89微摩尔),且无细胞毒性。这种抗增殖作用是由G2+M期的有丝分裂停滞介导的,不影响DNA合成,并且似乎与这些药物与外周型苯二氮䓬受体的特异性相互作用无关。

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