Improved synthesis of anxiolytic, anticonvulsant, and antinociceptive α2/α3-GABA (A)-ergic receptor subtype selective ligands as promising agents to treat anxiety …
An improved synthesis of the anxiolytic, anticonvulsant, and antinociceptive compounds: Hz-
166, and its bioisosteres 1, 2, 4-oxadiazole (MP-III-080) and 1, 3-oxazole (KRM-II-81) were …
166, and its bioisosteres 1, 2, 4-oxadiazole (MP-III-080) and 1, 3-oxazole (KRM-II-81) were …
Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics …
MM Poe, KR Methuku, G Li, AR Verma… - Journal of medicinal …, 2016 - ACS Publications
1, 4-Benzodiazepines are used in the treatment of anxiety disorders but have limited long-
term use due to adverse effects. HZ-166 (2) has been shown to have anxiolytic-like effects …
term use due to adverse effects. HZ-166 (2) has been shown to have anxiolytic-like effects …
[HTML][HTML] Design, synthesis and characterization of novel gamma‑aminobutyric acid type A receptor ligands
Antinociceptive ligand HZ-166 is a GABA A α2/α3 receptor subtype-selective potentiator. It
has been shown to exhibit anxiolytic-like effects in rodent and rhesus monkeys, as well as …
has been shown to exhibit anxiolytic-like effects in rodent and rhesus monkeys, as well as …
Synthesis and Pharmacological Evaluation of Novel GABAA Subtype Receptor Ligands with Potential Anxiolytic‐like and Anti‐hyperalgesic Effect
G Guerrini, G Ciciani, L Crocetti… - Journal of …, 2017 - Wiley Online Library
The identification of selective benzodiazepine site ligands, endowed with anxiolytic and anti‐
hyperalgesic action, is a relevant opportunity for the treatment of pain syndromes …
hyperalgesic action, is a relevant opportunity for the treatment of pain syndromes …
Hydrochloride salt of the GABAkine KRM-II-81
Imidazodiazepine (5-(8-ethynyl-6-(pyridin-2-yl)-4 H-benzo [f] imidazole [1, 5-α][1, 4] diazepin-
3-yl) oxazole or KRM-II-81) is a potentiator of GABAA receptors (a GABAkine) undergoing …
3-yl) oxazole or KRM-II-81) is a potentiator of GABAA receptors (a GABAkine) undergoing …
A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety
RT Lewis, WP Blackaby, T Blackburn… - Journal of medicinal …, 2006 - ACS Publications
The development of a series of GABAA α2/α3 subtype selective pyridazine based
benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is …
benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is …
Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo [f] imidazo [1, 5-a][1, 4] diazepine-3-carboxylate (HZ-166) as novel alpha 2, 3 selective potentiators of GABAA …
JM Witkin, JL Smith, X Ping, SD Gleason, MM Poe… - …, 2018 - Elsevier
HZ-166 has previously been characterized as an α2, 3-selective GABA A receptor modulator
with anticonvulsant, anxiolytic, and anti-nociceptive properties but reduced motor effects. We …
with anticonvulsant, anxiolytic, and anti-nociceptive properties but reduced motor effects. We …
Design, synthesis, and pharmacological evaluation of novel 1, 2, 4-triazol-3-amine derivatives as potential agonists of GABAA subtype receptors with anticonvulsant …
In the current study, a series of novel 1, 2, 4-triazol-3-amine derivatives were designed,
synthesized, and biologically evaluated in vivo for their anticonvulsant and hypnotic effects …
synthesized, and biologically evaluated in vivo for their anticonvulsant and hypnotic effects …
Augmentation of GABAergic neurotransmission by novel N-(substituted)-2-[4-(substituted) benzylidene] hydrazinecarbothioamides—a potential anticonvulsant …
L Tripathi, P Kumar - European journal of medicinal chemistry, 2013 - Elsevier
New N-(substituted)-2-[4-(substituted) benzylidene] hydrazinecarbothioamides were
designed, synthesized and evaluated for anticonvulsant activity and neurotoxicity. The …
designed, synthesized and evaluated for anticonvulsant activity and neurotoxicity. The …
Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1, 4, 5, 7-tetrahydropyrazolo [3, 4-b] pyridin-6-ones as potential hypnotic drugs
JL Falcó, M Lloveras, I Buira, J Teixidó, JI Borrell… - European journal of …, 2005 - Elsevier
Among the known non-benzodiazepinic hypnotic drugs acting on the α1 subunit of the
GABA-A receptor, Zolpidem (2a), Zaleplon (1b) and Indiplon (1a) have showed high affinity …
GABA-A receptor, Zolpidem (2a), Zaleplon (1b) and Indiplon (1a) have showed high affinity …