@article{a7edc08072f311df928f000ea68e967b,
title = "Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands: synthesis, pharmacology, and structure-activity relationships",
abstract = "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.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "M{\o}ller, {Henriette A} and Tommy Sander and Kristensen, {Jesper Langgaard} and Birgitte Nielsen and Jacob Krall and Bergmann, {Marianne Lerb{\ae}k} and Bolette Christiansen and Thomas Balle and Jensen, {Anders Asbj{\o}rn} and Fr{\o}lund, {Bente Flensborg}",
note = "Keywords: Animals; Cell Line; GABA Antagonists; GABA Plasma Membrane Transport Proteins; Humans; Hydrophobicity; Ligands; Membrane Potentials; Models, Molecular; Piperidines; Pyrazoles; Rats; Receptors, GABA-A; Structure-Activity Relationship; Synaptic Membranes",
year = "2010",
month = apr,
day = "22",
doi = "10.1021/jm100106r",
language = "English",
volume = "53",
pages = "3417--3421",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "8",
}