Imidazo[1,2-b]pyridazines. XXII. Syntheses of Some 2-Aryl-3-methoxy-6-(pyridinylmethylthio and pyridinylmethylamino)imidazo[1,2-b]pyridazines and Their Interaction with Central and Mitochondrial (Peripheral-Type) Benzodiazepine Receptors
- 1 January 1997
- journal article
- research article
- Published by CSIRO Publishing in Australian Journal of Chemistry
- Vol. 50 (2) , 91-96
- https://doi.org/10.1071/c96136
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).Keywords
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