Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands: synthesis, pharmacology, and structure-activity relationships
Research output: Contribution to journal › Journal article › Research › peer-review
A series of substituted 1-hydroxypyrazole analogues of the GABA(A) receptor partial agonist 5-(4-piperidyl)-3-isoxazolol (4-PIOL) have been synthesized and pharmacologically characterized. Several of the analogues displayed K(i) in the low nanomolar range at the native GABA(A) receptors and potent antagonism of the alpha(1)beta(2)gamma(2) receptor. It appears that several regions situated in proximity to the core of the orthosteric binding site of the GABA(A) receptor are able to accommodate large hydrophobic substituents.
| Original language | English |
|---|---|
| Journal | Journal of Medicinal Chemistry |
| Volume | 53 |
| Issue number | 8 |
| Pages (from-to) | 3417-3421 |
| ISSN | 0022-2623 |
| DOIs | |
| Publication status | Published - 2010 |
Bibliographical 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
- Former Faculty of Pharmaceutical Sciences
Research areas
ID: 20197322