GABAkines–Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors
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 …
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …
Measuring behavior in the home cage: study design, applications, challenges, and perspectives
F Grieco, BJ Bernstein, B Biemans… - Frontiers in behavioral …, 2021 - frontiersin.org
The reproducibility crisis (or replication crisis) in biomedical research is a particularly
existential and under-addressed issue in the field of behavioral neuroscience, where, in …
existential and under-addressed issue in the field of behavioral neuroscience, where, in …
The imidazodiazepine, KRM-II-81: an example of a newly emerging generation of GABAkines for neurological and psychiatric disorders
GABAkines, or positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors,
are used for the treatment of anxiety, epilepsy, sleep, and other disorders. The search for …
are used for the treatment of anxiety, epilepsy, sleep, and other disorders. The search for …
Preclinical research in paclitaxel-induced neuropathic pain: a systematic review
C Bacalhau, JT Costa-Pereira… - Frontiers in Veterinary …, 2023 - frontiersin.org
Introduction Chemotherapy-induced peripheral neuropathy (CIPN) is a common
consequence of cancer treatment and pain is a frequent complaint of the patients. Paclitaxel …
consequence of cancer treatment and pain is a frequent complaint of the patients. Paclitaxel …
Therapeutic effects of KRM-II-81, positive allosteric modulator for α2/3 subunit containing GABAA receptors, in a mouse model of Dravet syndrome
S Nakakubo, Y Hiramatsu, T Goto, S Kimura… - Frontiers in …, 2023 - frontiersin.org
Introduction: Dravet syndrome (DS) is an intractable epilepsy syndrome concomitant with
neurodevelopmental disorder that begins in infancy. DS is dominantly caused by mutations …
neurodevelopmental disorder that begins in infancy. DS is dominantly caused by mutations …
Synergistic antihyperalgesic and antinociceptive effects of morphine and methyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate (MP-III-024): a positive …
Abstract Rationale Opioid and GABA A receptors are both located in central nociceptive
pathways, and compounds that activate these receptors have pain-relieving properties. To …
pathways, and compounds that activate these receptors have pain-relieving properties. To …
Protein phosphatase 2A inhibitors: a possible pharmacotherapy for benzodiazepine dependence
C Kobayashi, N Kitanaka, M Nakai… - Journal of Pharmacy …, 2024 - academic.oup.com
Abstract Objectives Benzodiazepines (BZDs) activate the γ-aminobutyric acid (GABA)
subtype A (GABAA) receptors, and thus are widely used medicines for the treatment of …
subtype A (GABAA) receptors, and thus are widely used medicines for the treatment of …
Metabolism, pharmacokinetics, and anticonvulsant activity of a deuterated analog of the α2/3‐selective GABAkine KRM‐II‐81
Abstract The imidazodiazepine,(5‐(8‐ethynyl‐6‐(pyridin‐2‐yl)‐4H‐benzo [f] imidazole [1, 5‐
α][1, 4] diazepin‐3‐yl) oxazole or KRM‐II‐81) is a new α2/3‐selective GABAkine (gamma …
α][1, 4] diazepin‐3‐yl) oxazole or KRM‐II‐81) is a new α2/3‐selective GABAkine (gamma …
BAER‐101, a selective potentiator of α2‐ and α3‐containing GABAA receptors, fully suppresses spontaneous cortical spike‐wave discharges in Genetic Absence …
A MacLean, AS Chappell, J Kranzler… - Drug Development …, 2024 - Wiley Online Library
Abstract BAER‐101 (formerly AZD7325) is a selective partial potentiator of α2/3‐containing γ‐
amino‐butyric acid A receptors (GABAARs) and produces minimal sedation and dizziness …
amino‐butyric acid A receptors (GABAARs) and produces minimal sedation and dizziness …
KRM–II–81 suppresses epileptifom activity across the neural network of cortical tissue from a patient with pharmacoresistant epilepsy
A clinical case of a 19-year-old male patient with pharmacoresistant seizures occurring
following parieto-occipital tumor-resection at age 6 is described. Seizure surgery work-up …
following parieto-occipital tumor-resection at age 6 is described. Seizure surgery work-up …