Benzodiazepine antagonist flumazenil reduces bicuculline-induced enhancement of neuronal activity in the spinal cord.

Neuropharmacology

Pharma Research Department, F. Hoffmann-La Roche Ltd, Basel, Switzerland.

Published: January 1991

The interaction between the GABAA receptor antagonist bicuculline and the benzodiazepine receptor (BR) antagonist flumazenil was studied in the lumbosacral cord of spinal cats. Bicuculline (0.8 mg/kg i.v.) evoked epileptiform bursting of motoneurons in parallel with a depression of peripherally elicited dorsal root potentials (DRP) and dorsal root reflexes (DDR). A low dose of flumazenil (0.03 mg/kg i.v.) reduced the bursting activity of motoneurons as well as partially reversed the depression of DRP and DRR induced by bicuculline. It is suggested that an endogenous BR ligand down-regulating GABAA receptors is released during the bicuculline-evoked enhancement of neuronal activity and may contribute to the epileptiform discharge of motoneurons in the spinal cord.

Download full-text PDF

Source
http://dx.doi.org/10.1016/0028-3908(91)90051-cDOI Listing

Publication Analysis

Top Keywords

antagonist flumazenil
8
enhancement neuronal
8
neuronal activity
8
spinal cord
8
receptor antagonist
8
dorsal root
8
benzodiazepine antagonist
4
flumazenil reduces
4
reduces bicuculline-induced
4
bicuculline-induced enhancement
4

Similar Publications

Mimosa tenuiflora ("jurema-preta") is traditionally used in folk medicine for various diseases. The study investigated the neuropharmacological potential of Mimosa tenuiflora bark fraction (FATEM) in adult zebrafish. This included the acute toxicity (LC50) of FATEM (0.

View Article and Find Full Text PDF

Anxiogenic-like effects of coumarin, possibly through the GABAkine interaction pathway: Animal studies with in silico approaches.

Behav Brain Res

March 2025

Department of Pharmacy, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, Bangladesh; Bioinformatics and Drug Innovation Laboratory, BioLuster Research Center Ltd., Gopalganj 8100, Bangladesh; Pharmacy Discipline, Khulna University, Khulna 9208, Bangladesh. Electronic address:

Background: Anxiety disorder is the most common mental illness and a major contributor to impairment. Thus, there is an urgent need to find novel lead compounds to mitigate anxiety. It is widely recognized that the neurobiology of anxiety-related behavior involves GABAergic systems.

View Article and Find Full Text PDF

Plant-based components have helped generate novel lead molecules and scaffolds for anxiety research in psychopharmacology. The present study examined the anxiolytic properties of sesamol (SES), a phenolic lignan derived from Sesamum indicum, employing both in vivo and computational methods to understand its mechanisms of action. In this experiment, adult Swiss albino mice received various doses of SES (25 and 50 mg/kg, p.

View Article and Find Full Text PDF

This study investigated the anxiolytic and anticonvulsant effects and safety profile of limonene enantiomers and their oxidized derivatives. The toxicity test was performed by monitoring the animals for 96 hours, with no deaths or significant toxicity observed up to the highest dose, which allowed the determination of the LD50. Doses of 4, 20 and 40 mg/kg were tested, with no toxicity observed up to 96 h (LD50>40 mg/kg).

View Article and Find Full Text PDF

Alternative Reinforcers Enhance the Effects of Opioid Antagonists, but Not Agonists, on Oxycodone Choice Self-Administration in Nonhuman Primates.

J Pharmacol Exp Ther

October 2024

Behavioral Neuroimaging Laboratory, McLean Hospital, Belmont, Massachusetts (F.B.d.M., S.J.K.) and Department of Psychiatry, Harvard Medical School, Boston, Massachusetts (F.B.d.M., S.J.K.)

Clinical reports suggest that the most effective strategies for managing opioid use disorder comprise a comprehensive treatment program of both pharmacological and nonpharmacological approaches. However, the conditions under which these combinations are most effective are not well characterized. This study examined whether the presence of an alternative reinforcer could alter the efficacy of Food and Drug Administration-approved opioid antagonist or agonist medications, as well as the nonopioid flumazenil, in decreasing oxycodone choice self-administration in nonhuman primates.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!