SIGMA-RECEPTOR-ACTIVE NEUROLEPTICS ARE CYTOTOXIC TO C6 GLIOMA-CELLS IN CULTURE

被引：74

作者：

VILNER, BJ ^{[1
]}

BOWEN, WD ^{[1
]}

机构：

[1] NIDDK,MED CHEM LAB,RECEPTOR BIOCHEM & PHARMACOL UNIT,BLDG 8,RM B1-23,9000 ROCKVILLE PIKE,BETHESDA,MD 20892

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1993年 / 244卷 / 02期

关键词：

SIGMA-RECEPTORS; ANTIPSYCHOTIC DRUGS; CYTOTOXICITY;

D O I：

10.1016/0922-4106(93)90029-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

When exposed to neuroleptics (100 mum), C6 glioma cells exhibited marked changes in cell morphology, accompanied by cessation of cell division and ultimately cell death. The degree of activity generally correlated with binding affinity at sigma sites: fluphenazine = perphenazine = haloperidol = reduced haloperidol > pimozide = spiperone much greater than much greater than (-)-sulpiride. Sigma-inactive compounds (100 muM) which block dopamine, serotonin, phencyclidine, muscarinic receptors and adrenoceptors showed no effect. These results may suggest a role of sigma binding sites in maintenance of cell viability.

引用

页码：199 / 201

页数：3

共 8 条

[1] METABOLITES OF HALOPERIDOL DISPLAY PREFERENTIAL ACTIVITY AT SIGMA-RECEPTORS COMPARED TO DOPAMINE D-2 RECEPTORS [J].

BOWEN, WD ;

MOSES, EL ;

TOLENTINO, PJ ;

WALKER, JM .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 177 (03) :111-118

[2]

BOWEN WD, 1992, MULTIPLE SIGMA PCP R, P155

[3] A PROPOSAL FOR THE CLASSIFICATION OF SIGMA BINDING-SITES [J].

QUIRION, R ;

BOWEN, WD ;

ITZHAK, Y ;

JUNIEN, JL ;

MUSACCHIO, JM ;

ROTHMAN, RB ;

SU, TP ;

TAM, SW ;

TAYLOR, DP .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1992, 13 (03) :85-86

[4]

SU TP, 1982, J PHARMACOL EXP THER, V223, P284

[5] SIGMA-OPIATES AND CERTAIN ANTIPSYCHOTIC-DRUGS MUTUALLY INHIBIT (+)-[H-3]SKF-10,047 AND [H-3]HALOPERIDOL BINDING IN GUINEA-PIG BRAIN MEMBRANES [J].

TAM, SW ;

COOK, L .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1984, 81 (17) :5618-5621

[6]

Vilner B. J., 1992, Society for Neuroscience Abstracts, V18, P22

[7]

VILNER BJ, 1992, MULTIPLE SIGMA PCP R, P341

[8]

WALKER JM, 1990, PHARMACOL REV, V42, P355

← 1 →