GABAkines–Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors

A Lippa, MM Poe, JL Smith, X Jin, X Ping… - Pharmacology & …, 2022 - Elsevier
Positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors or GABAkines
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …

Sex differences in neuroimmune and glial mechanisms of pain

AM Gregus, IS Levine, KA Eddinger, TL Yaksh… - Pain, 2021 - journals.lww.com
Pain is the primary motivation for seeking medical care. Although pain may subside as
inflammation resolves or an injury heals, it is increasingly evident that persistency of the pain …

Positive interaction between GPER and β-alanine in the dorsal root ganglion uncovers potential mechanisms: mediating continuous neuronal sensitization and …

Z Xu, W Xie, Y Feng, Y Wang, X Li, J Liu… - Journal of …, 2022 - Springer
Background The pathogenesis of neuropathic pain and the reasons for the prolonged
unhealing remain unknown. Increasing evidence suggests that sex oestrogen differences …

[HTML][HTML] Current status of GABA receptor subtypes in analgesia

X Qian, X Zhao, L Yu, Y Yin, XD Zhang, L Wang… - Biomedicine & …, 2023 - Elsevier
Abstract Gamma-aminobutyric acid (GABA), a non-protein-producing amino acid
synthesized from the excitatory amino acid glutamate via the enzyme glutamic acid …

Sex differences in pain along the neuraxis

P Presto, M Mazzitelli, R Junell, Z Griffin… - …, 2022 - Elsevier
Despite the overwhelming female-predominance in chronic pain disorders, preclinical pain
studies have historically excluded females as research subjects. Male-biased explanations …

[HTML][HTML] Epigenetic landscapes of pain: DNA methylation dynamics in chronic pain

HY Xiong, A Wyns, JV Campenhout, J Hendrix… - International Journal of …, 2024 - mdpi.com
Chronic pain is a prevalent condition with a multifaceted pathogenesis, where epigenetic
modifications, particularly DNA methylation, might play an important role. This review delves …

Sex-dependent antiallodynic effect of α2 adrenergic receptor agonist tizanidine in rats with experimental neuropathic pain

EJ Rodríguez-Palma, DG Castelo-Flores… - European Journal of …, 2022 - Elsevier
The purpose of this study was to investigate the mechanism of antiallodynic effect of
tizanidine in neuropathic rats. Spinal nerve ligation reduced withdrawal threshold which was …

Prepubescent female rodents have enhanced hippocampal LTP and learning relative to males, reversing in adulthood as inhibition increases

AA Le, JC Lauterborn, Y Jia, W Wang, CD Cox… - Nature …, 2022 - nature.com
Multiple studies indicate that adult male rodents perform better than females on spatial
problems and have a lower threshold for long-term potentiation (LTP) of hippocampal CA3 …

Activation of α6-containing GABAA receptors induces antinociception under physiological and pathological conditions

EJ Rodríguez-Palma, E Yarim, AM Islas-Espinoza… - Pain, 2023 - journals.lww.com
The loss of GABAergic inhibition is a mechanism that underlies neuropathic pain. Therefore,
rescuing the GABAergic inhibitory tone through the activation of GABA A receptors is a …

Enhancing cognitive recovery in chronic traumatic brain injury through simultaneous allosteric modulation of α7 nicotinic acetylcholine and α5 GABAA receptors

AF Balleste, A Sangadi, DJ Titus, T Johnstone… - Experimental …, 2024 - Elsevier
Traumatic brain injury (TBI) leads to changes in the neural circuitry of the hippocampus that
result in chronic learning and memory deficits. However, effective therapeutic strategies to …