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 …
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 …
The α2, 3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats
JM Witkin, R Cerne, PG Davis, KB Freeman… - Pharmacology …, 2019 - Elsevier
Clinical evidence indicates that positive allosteric modulators (PAMs) of GABA A receptors
have analgesic benefit in addition to efficacy in anxiety disorders. However, the utility of …
have analgesic benefit in addition to efficacy in anxiety disorders. However, the utility of …
Allosteric GABAA Receptor Modulators—A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility
BA Vega Alanis, MT Iorio, LL Silva, K Bampali, M Ernst… - Molecules, 2020 - mdpi.com
GABAA receptor modulators are structurally almost as diverse as their target protein. A
plethora of heterocyclic scaffolds has been described as modulating this extremely important …
plethora of heterocyclic scaffolds has been described as modulating this extremely important …
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies
The pharmacological actions exerted by benzodiazepines are dependent on the discrete α
protein subunits of the γ-aminobutyric acid type A receptor (GABA AR). Recent …
protein subunits of the γ-aminobutyric acid type A receptor (GABA AR). Recent …
The α2, 3-selective potentiators of GABAA receptors, KRM-II-81 and MP-III-80, produce anxiolytic-like effects and block chemotherapy-induced hyperalgesia in mice …
Opiate analgesics are one of the treatment options for severe chronic pain, including late-
stage cancer, chronic back pain and other disorders. The recent resurgence in opioid …
stage cancer, chronic back pain and other disorders. The recent resurgence in opioid …
Improved scale-up synthesis and purification of clinical asthma candidate MIDD0301
We report an improved and scalable synthesis of MIDD0301, a positive GABAA receptor
modulator that is under development as oral and inhaled treatments for asthma. In contrast …
modulator that is under development as oral and inhaled treatments for asthma. In contrast …
Imidazodiazepine anticonvulsant, KRM-II-81, produces novel, non-diazepam-like antiseizure effects
The need for improved medications for the treatment of epilepsy and chronic pain is
essential. Epileptic patients typically take multiple antiseizure drugs without complete …
essential. Epileptic patients typically take multiple antiseizure drugs without complete …
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 …
Synthesis, spectral, crystal, computational studies and antimicrobial activities of (E)-N-(substituted arylidene)-3-(trifluoromethyl) anilines
N Dineshkumar, I Muthuvel, G Thirunarayanan - 2023 - nopr.niscpr.res.in
A series of (E)-N-(substituted arylidene)-3-(trifluoromethyl) anilines have been synthesised
by ZnFe2O4 catalyzed microwave promoted condensation of 3-trifluoromethyl aniline and …
by ZnFe2O4 catalyzed microwave promoted condensation of 3-trifluoromethyl aniline and …