High doses of penicillin decreases [3H]flunitrazepam binding sites in rat neuron primary culture.

Abstract:

:Penicillin (PC) neurotoxicity (convulsions and encephalopathy) is considered to be due to GABAergic inhibition. The effects of penicillin G(PCG) on [3H]flunitrazepam (FNZ) binding in rat neuron-enriched primary cultures was examined to assess the role of the benzodiazepine (BDZ) receptor in the neurotoxicity. PCG application for 24 h induced a significant decrease in [3H]FNZ binding activity at 10(-3) M, and a decrease in available receptor number (Bmax) at 10(-2) M, without obvious cell damage. Pre-application of the BDZ receptor antagonist, Ro-15-1788, prevented the PC-induced decrease in [3H]FNZ binding activity. Therefore, PC seems to reduce the number of BDZ receptors through a direct effect on this receptor, which is a part of the major inhibitory system in mammalian brain; the GABAergic macromolecular receptor complex. This decrease in BDZ receptors may play a role in PC-induced neurotoxicity, especially encephalopathy.

journal_name

Brain Dev

journal_title

Brain & development

authors

Shiraishi H,Ito M,Go T,Mikawa H

doi

10.1016/0387-7604(93)90121-n

subject

Has Abstract

pub_date

1993-09-01 00:00:00

pages

356-61

issue

5

eissn

0387-7604

issn

1872-7131

pii

0387-7604(93)90121-N

journal_volume

15

pub_type

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