Gabaergic Drugs

GABAergic drugs are medications that enhance, mimic, or otherwise modify signaling by gamma-aminobutyric acid (GABA), the principal inhibitory neurotransmitter in the central nervous system. They reduce neuronal excitability by increasing GABA-mediated inhibition, commonly through GABA-A receptor chloride channels or GABA-B receptor pathways that regulate ion conductance through G proteins. This pharmacological class includes benzodiazepines, barbiturates, gabapentinoids, and other agents used to treat anxiety, insomnia, epilepsy, muscle spasticity, and related disorders. Understanding their receptor selectivity, onset, duration, and adverse effects supports safer prescribing and informs the development of therapies with improved clinical benefits and reduced sedation, tolerance, or dependence.

Gabaergic Drugs - Related Videos

Education

JoVE Core - Pharmacology

Antiepileptic Drugs: GABAergic Pathway Potentiators

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2024

γ-aminobutyric acid or GABA, plays a pivotal role as an inhibitory neurotransmitter in the brain. GABA pathway potentiators, also known as GABAergic drugs, are a class of pharmaceutical agents designed to enhance the functioning of the GABAergic system. These medications primarily treat epilepsy, a neurological disorder characterized by recurrent seizures. The key GABA pathway potentiators used in epilepsy management are as follows. Benzodiazepines are a well-known class of drugs used for their...

Research

JoVE Journal - Medicine
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Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

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Cited by 4 •

2016

Here we describe a protocol using the web-based drug repurposing hypothesis generation tool: "RE:fine Drugs." This protocol can be modified to a user's preferences at the level of the query type (gene, drug or disease) and/or the range of available advanced options.

Research

JoVE Journal - Neuroscience
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A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

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Cited by 5 •

2019

A validated computerized battery of neuropsychological and neurophysiological tests is used to study pharmacodynamic effects on the central nervous system of newly developed drugs in early phase development. To demonstrate the test battery, the acute effects of mecamylamine and the reversal of these effects by two agonist drugs are described.

Drug toxicity: Drug–Drug Interaction

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2026

Drug–drug interactions can precipitate toxicity through multiple mechanisms. Absorption interactions alter how drugs enter the body, exemplified when ranitidine increases the absorption of basic drugs, while cholestyramine decreases the levels of propranolol. Protein binding interactions occur when drugs share the same binding sites on plasma proteins. Drugs like aspirin and warfarin, when bound in excess, can lead to increased free drug concentrations, enhancing the potential for...

The Mesenteric Lymph Duct Cannulated Rat Model: Application to the Assessment of Intestinal Lymphatic Drug Transport

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Cited by 48 •

2015

Here we describe a technique to cannulate the mesenteric lymph duct in rats which enables quantification of lipid and drug transport via the lymphatic system following intestinal delivery. The technique can be adapted to assess mesenteric lymph concentrations and/or transport of fluid, immune cells, peptides, proteins and lipophilic molecules.

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