Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands: synthesis, pharmacology, and structure-activity relationships
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands : synthesis, pharmacology, and structure-activity relationships. / Møller, Henriette A; Sander, Tommy; Kristensen, Jesper Langgaard; Nielsen, Birgitte; Krall, Jacob; Bergmann, Marianne Lerbæk; Christiansen, Bolette; Balle, Thomas; Jensen, Anders Asbjørn; Frølund, Bente Flensborg.
I: Journal of Medicinal Chemistry, Bind 53, Nr. 8, 2010, s. 3417-3421.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acidA receptor ligands
T2 - synthesis, pharmacology, and structure-activity relationships
AU - Møller, Henriette A
AU - Sander, Tommy
AU - Kristensen, Jesper Langgaard
AU - Nielsen, Birgitte
AU - Krall, Jacob
AU - Bergmann, Marianne Lerbæk
AU - Christiansen, Bolette
AU - Balle, Thomas
AU - Jensen, Anders Asbjørn
AU - Frølund, Bente Flensborg
N1 - 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
PY - 2010
Y1 - 2010
N2 - 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.
AB - 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.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1021/jm100106r
DO - 10.1021/jm100106r
M3 - Journal article
C2 - 20355712
VL - 53
SP - 3417
EP - 3421
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 8
ER -
ID: 20197322