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Imidazo[1,2‐ b ]pyridazines: Syntheses and interaction with central and peripheral‐type (mitochondrial) benzodiazepine receptors
Author(s) -
Barlin Gordon B.
Publication year - 1998
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570350515
Subject(s) - chemistry , receptor , benzodiazepine , gabaa receptor , peripheral , stereochemistry , pharmacology , biochemistry , medicine , biology
The fundamental chemistry of pyridazines, the syntheses of substituted irnidazo[1,2‐ b ]pyridazines (1) (and some related compounds) and the interaction of the products with central benzodiazepine receptors (CBR) and peripheral‐type (mitochondrial) benzodiazepine receptors (PBR) are described. Some of these imidazo[1,2‐ b ]pyridazines had high selective affinity for the central benzodiazepine receptors and others had high selectivity for the peripheral‐type (mitochondrial) benzodiazepine receptors. The results of structure‐activity 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 peripheral‐type (mitochondrial) benzodiazepine receptors are being examined as possible radiopharmaceuticals for imaging of tumors (and other disease states).