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Imidazo[1,2-b]pyridazines: Syntheses and interaction with central and peripheral-type (mitochondrial) benzodiazepine receptors
โ Scribed by Gordon B. Barlin
- Publisher
- Journal of Heterocyclic Chemistry
- Year
- 1998
- Tongue
- English
- Weight
- 900 KB
- Volume
- 35
- Category
- Article
- ISSN
- 0022-152X
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โฆ Synopsis
Abstract
The fundamental chemistry of pyridazines, the syntheses of substituted irnidazo[1,2โb]pyridazines (1) (and some related compounds) and the interaction of the products with central benzodiazepine receptors (CBR) and peripheralโtype (mitochondrial) benzodiazepine receptors (PBR) are described.
Some of these imidazo[1,2โb]pyridazines had high selective affinity for the central benzodiazepine receptors and others had high selectivity for the peripheralโtype (mitochondrial) benzodiazepine receptors. The results of structureโactivity studies and molecular modeling will be reported.
In vivo tests of some compounds which interacted strongly with the central benzodiazepine receptors revealed reasonably potent anticonvulsant/anticonflict activity, and some of those which bind selectively to the peripheralโtype (mitochondrial) benzodiazepine receptors are being examined as possible radiopharmaceuticals for imaging of tumors (and other disease states).
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