Author:
Barlin Gordon B.,Davies Les P.,Ireland Stephen J.,Ngu-Schwemlein Maria M. L.
Abstract
2-Aryl-3-methoxy-6-(pyridinylmethylthio and
pyridinylmethylamino)imidazo[1,2-b]pyridazines
have been prepared and examined as ligands for benzodiazepine receptors. Most
were highly effective in displacing
[3H]diazepam from central benzodiazepine
receptors present in rat brain membranes but showed little capacity for its
displacement from mitochondrial (peripheral-type) benzodiazepine receptors
present in rat kidney membranes. For example,
3-methoxy-2-(3′,4′-methylenedioxyphenyl)-6-(pyridin-2′′-ylmethylthio)imidazo[1,2-b]pyridazine
had an IC50 value of 1 · 7 nM for central
receptors but gave only 39% displacement at 1000 nM for mitochondrial
receptors.
Of all the compounds described in this series of papers,
3-methoxy-6-(2′-methoxybenzylamino)-2-(3′′,4′′-methylenedioxyphenyl)imidazo[1,2-b]pyridazine
was the most active in displacing [3H]diazepam
from central receptors (IC50 0·3 nM), and it had
a low affinity for mitochondrial receptors (40% displacement of
[3H]diazepam at 1000 nM).
Cited by
10 articles.
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