Premium
Antiproliferative Action of Benzodiazepines in Cultured Brain Cells Is Not Mediated Through the Peripheral‐Type Benzodiazepine Acceptor
Author(s) -
Gorman Adrienne M. C.,
O'Beirne Gerard B.,
Regan Ciaran M.,
Williams D. Clive
Publication year - 1989
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1989.tb11782.x
Subject(s) - benzodiazepine , diazepam , clonazepam , cell culture , neuroblastoma , binding site , cell growth , affinities , pharmacology , chemistry , mechanism of action , cell type , cell , biology , in vitro , receptor , biochemistry , genetics
The benzodiazepines, Ro 5–4864, diazepam, clonazepam, and also PK‐11195, inhibited, at micromolar concentrations, the proliferation of rat C 6 glioma and mouse neuro‐2A neuroblastoma cells in culture. The cells possessed high levels of “peripheral‐type” high‐affinity benzodiazepine binding sites as judged by binding assays and displacement potencies. However, the different potencies and specificities of compounds for the antiproliferative actions and binding affinities for the binding site suggest that the antiproliferative actions were not mediated through the peripheral‐type binding site. In support of this, these compounds have also been shown to inhibit proliferation of some nonneuronal cultured cell lines, e.g., mouse SP2/0‐Agl4 hybridoma and rat NCTC epithelial cells, which have no detectable high‐affinity peripheral‐type benzodiazepine binding sites.