The beta-carboline ZK 93423 inhibits reticulata neurons: an effect reversed by benzodiazepine antagonists.

Abstract:

:A novel beta-carboline with benzodiazepine-like properties has recently been synthesized. We compared the effect of the i.v. administration of this drug, ZK 93423, with diazepam on the activity of nigral pars reticulata neurons which are known to be very sensitive to the inhibitory effect produced by GABA-mimetics and benzodiazepines. ZK 93423 (0.05-1.0 mg/kg) inhibited reticulata cells in a dose-related manner up to the cessation of their activity. Since the maximal rate-inhibition elicited by diazepam (1.0 mg/kg) was some 55% of baseline, ZK 93423 showed a much greater potency. Moreover, the firing depression by ZK 93423 was prevented and reversed by two benzodiazepine receptor antagonists: Ro15-1788 and ZK 93426. However, the dosage of Ro15-1788 required for these actions was at least five times higher than that for the blockade of the diazepam effect. The results indicate that the beta-carboline agonist ZK 93423 decreases the activity of reticulata neurons more effectively than diazepam.

journal_name

Life Sci

journal_title

Life sciences

authors

Mereu G,Corda MG,Carcangiu P,Giorgi O,Biggio G

doi

10.1016/0024-3205(87)90333-x

subject

Has Abstract

pub_date

1987-04-06 00:00:00

pages

1423-30

issue

14

eissn

0024-3205

issn

1879-0631

pii

0024-3205(87)90333-X

journal_volume

40

pub_type

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