Identification of a New Pyrazolo[1,5-a]quinazoline Ligand Highly Affine to γ-Aminobutyric Type A (GABAA) Receptor Subtype with Anxiolytic-Like and Antihyperalgesic Activity
作者： Gabriella Guerrini , Giovanna Ciciani , Letizia Crocetti , Simona Daniele , Carla Ghelardini
DOI: 10.1021/ACS.JMEDCHEM.7B01151
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摘要: Compounds that can act on GABAA receptor subtype in a selective manner, without the side effects of classical benzodiazepine ligands, represent promising therapeutic tools neurological disorder as well for relief pain or comorbidity anxiety states and depression. Continuing our research here is reported synthesis series pyrazolo[1,5-a]quinazoline 3- and/or 8-substituted 5-deaza analogues previous pyrazolo[5,1-c][1,2,4]benzotriazine, already identified ligands endowed with anxiolytic-like antihyperalgesic action enhancer cognition. Between new compounds stands out 12b its high affinity value (Ki = 0.27 nM) ability to relieve neuropathic painful conditions evaluated CCI STZ murine model.
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