1221275-01-9Relevant academic research and scientific papers
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as γ-aminobutyric acidA receptor ligands: Synthesis, pharmacology, and structure-activity relationships
Fr?lund, Bente,M?ller, Henriette A.,Sander, Tommy,Kristensen, Jesper L.,Nielsen, Birgitte,Krall, Jacob,Bergmann, Marianne L.,Christiansen, Bolette,Balle, Thomas,Jensen, Anders A.
supporting information; experimental part, p. 3417 - 3421 (2010/09/05)
A series of substituted 1-hydroxypyrazole analogues of the GABAA receptor partial agonist 5-(4-piperidyl)-3-isoxazolol (4-PIOL) have been synthesized and pharmacologically characterized. Several of the analogues displayed Ki in the low nanomolar range at the native GABA A receptors and potent antagonism of the α1β 2γ2 receptor. It appears that several regions situated in proximity to the core of the orthosteric binding site of the GABAA receptor are able to accommodate large hydrophobic substituents.
