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Pharmaceuticals
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Innovative Approaches to GABAergic Drug Discovery: From Molecular Mechanisms to...
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Innovative Approaches to GABAergic Drug Discovery: From Molecular Mechanisms to Advanced Therapeutics

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 25 February 2026 | Viewed by 1141

Special Issue Editors

Dr. Wojciech Kołodziejczyk

E-Mail Website
Guest Editor
Department of Chemistry, Physics and Atmospheric Sciences, Jackson State University, Jackson, MS 39217, USA
Interests: drug delivery; drug interactions; cannabinoids; legal highs; organic electronics; organic LED; perovskites
Dr. Donato Colangelo

E-Mail Website
Guest Editor
Department of Health Sciences, Università del Piemonte Orientale UPO, 28100 Novara, Italy
Interests: microenvironment; tumor targeting; pharmacokinetics; toxicology; telomerase; nanoparticles for drug delivery; chemotherapy; pharmacodynamics; inflammation; neurosciences in cancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue invites contributions that explore the role of gamma-aminobutyric acid (GABA) in drug discovery and development. GABAergic signaling plays a pivotal role in numerous neurological and psychiatric disorders, including epilepsy, anxiety, depression, and neurodegenerative diseases. Understanding the mechanisms of GABA receptor modulation and the development of GABA-targeting therapeutics is essential for advancing treatment strategies in these areas.

We welcome studies focused on GABA receptor pharmacology, ligand design, and novel approaches to modulating GABAergic activity. Of particular interest is work integrating computational methods—such as artificial intelligence, machine learning, and structural bioinformatics—with experimental strategies, including high-throughput screening and in vivo validation.

Research into innovative drug delivery systems that enhance the efficacy, targeting, and bioavailability of GABAergic drugs is also encouraged. This includes studies of nanoparticle-based systems, liposomal formulations, and polymeric carriers designed for controlled release.

Through this Special Issue, we aim to highlight cutting-edge research that deepens our understanding of GABA’s therapeutic potential and accelerates the development of next-generation GABAergic interventions. We invite original research articles, reviews, and case studies that contribute novel insights and technological advancements to this critical area of pharmaceutical science.

Dr. Wojciech Kołodziejczyk
Dr. Donato Colangelo
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • GABAergic signaling
  • GABA receptors
  • drug discovery
  • neurological and psychiatric disorders
  • ligand design
  • computational drug development
  • artificial intelligence in pharmacology
  • high-throughput screening
  • targeted drug delivery
  • controlled release systems

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Published Papers (2 papers)

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Review

19 pages, 2344 KB  
Review
Re-Evaluation of the Ultrastructural Localization of Tonic GABA-A Receptors
by Abraham Rosas-Arellano
Pharmaceuticals 2026, 19(1), 25; https://doi.org/10.3390/ph19010025 - 22 Dec 2025
Abstract
Cell membrane receptors play key roles in physiological and pathological processes, yet the mechanisms governing their expression and distribution across the plasma membrane remain not completely understood. Broadly, membrane receptors can be categorized into phasic and tonic receptors. Tonic GABA-A receptors have attracted [...] Read more.
Cell membrane receptors play key roles in physiological and pathological processes, yet the mechanisms governing their expression and distribution across the plasma membrane remain not completely understood. Broadly, membrane receptors can be categorized into phasic and tonic receptors. Tonic GABA-A receptors have attracted considerable interest due to their distinct molecular composition and their capacity to mediate highly sensitive, sustained inhibitory responses in the presence of ambient GABA. Traditionally, these receptors have been described as residing in peri- and extrasynaptic regions, where they are thought to sense GABA spillover and generate tonic inhibition. However, evidence accumulated over several decades has challenged this canonical view. Multiple studies have reported activity-dependent and pathology-associated relocalization of tonic GABA-A receptor subunits from their typical peri- and extrasynaptic domains into the synaptic cleft. This phenomenon has been documented in both in vivo and in vitro models, yet major questions remain regarding its occurrence, underlying mechanisms, functional significance, and adaptive value. This review synthesizes current evidence and highlights ongoing controversies surrounding the ultrastructural localization of tonic GABA-A receptors. Based on an exhaustive search of the PubMed database, this review summarizes key findings from studies investigating the subcellular distribution of these receptors and discusses emerging perspectives on their potential synaptic presence. Full article
(This article belongs to the Special Issue Innovative Approaches to GABAergic Drug Discovery: From Molecular Mechanisms to Advanced Therapeutics)
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25 pages, 1467 KB  
Review
Golexanolone Attenuates Neuroinflammation, Fatigue, and Cognitive and Motor Impairment in Diverse Neuroinflammatory Disorders
by Marta Llansola, Gergana Mincheva, Yaiza M. Arenas, Paula Izquierdo-Altarejos, Maria A. Pedrosa, Thomas P. Blackburn, Torbjörn Bäckström, Bruce F. Scharschmidt, Magnus Doverskog and Vicente Felipo
Pharmaceuticals 2025, 18(11), 1757; https://doi.org/10.3390/ph18111757 - 18 Nov 2025
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Abstract
Background and Objectives: Neuroinflammation plays a significant role in liver and neurological disorders via its disruption of neurotransmission, which alters cerebral function, resulting in cognitive and motor impairment, fatigue, anxiety, and depression. A key interaction exists between GABAergic neurotransmission and neuroinflammation, whereby [...] Read more.
Background and Objectives: Neuroinflammation plays a significant role in liver and neurological disorders via its disruption of neurotransmission, which alters cerebral function, resulting in cognitive and motor impairment, fatigue, anxiety, and depression. A key interaction exists between GABAergic neurotransmission and neuroinflammation, whereby excessive GABAA receptor activation exacerbates cognitive and behavioural impairment. Golexanolone, a novel GABAA-receptor-modulating steroid antagonist (GAMSA), primarily attenuates GABAergic potentiation via GABAA-positive steroid allosteric receptor modulators such as allopregnanolone. This review aims to summarize new evidence showing that golexanolone improves peripheral inflammation, neuroinflammation, and neurological alterations in animal models of different neurological pathologies. We provide an overview of the first clinical trial using this novel compound. Results: In rat models of hyperammonemia and minimal hepatic encephalopathy (MHE), peripheral inflammation induces microglia and astrocyte activation and neuroinflammation, altering GABAergic neurotransmission and resulting in cognitive and motor impairment. Golexanolone’s unique dual action reduces peripheral inflammation and glial activation, thus normalizing neurotransmission and cognitive and motor function. Furthermore, a phase II study in cirrhotic patients with MHE shows that golexanolone is well tolerated and improves cognition. Similarly, in a model of primary biliary cholangitis (PBC) involving bile-duct ligation, peripheral inflammation, neuroinflammation, and altered neurotransmission—associated with fatigue, impaired memory, and locomotor gait and motor incoordination—were reversed by the dual action of golexanolone. In the Parkinson’s disease (PD) rat model induced by neurotoxin 6-OHDA, rats exhibited fatigue, anhedonia, impaired memory, and locomotor gait and motor incoordination, which were associated with microglia and astrocyte activation in the substantia nigra and striatum, in addition to tyrosine hydroxylase (TH) loss. Golexanolone reduces microglia and astrocyte activation, partially reduces TH loss, and improves fatigue, anhedonia, memory, locomotor gait, and motor incoordination. Golexanolone also normalizes elevated levels of α-synuclein. Conclusions: These findings suggest that golexanolone has beneficial therapeutic effects for treating fatigue, depression, motor, and cognitive impairment across diverse neuroinflammatory conditions, including synucleinopathies. Full article
(This article belongs to the Special Issue Innovative Approaches to GABAergic Drug Discovery: From Molecular Mechanisms to Advanced Therapeutics)
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