
TY  - JOUR
A1  - Barlin, Gordon B. 
A1  - Davies, Les P. 
A1  - Ireland, Stephen J. 
A1  - Ngu-Schwemlein, Maria M. L. 
T1  - Imidazo[1,2-<emph type="2">b</emph>]pyridazines. XXII. Syntheses of Some 2-Aryl-3-methoxy-6-(pyridinylmethylthio and pyridinylmethylamino)imidazo[1,2-<emph type="2">b</emph>]pyridazines and Their Interaction with Central and Mitochondrial (Peripheral-Type) Benzodiazepine Receptors
JF  - Australian Journal of Chemistry
JO  - Aust. J. Chem.
Y1  - 1997
VL  - 50
IS  - 2
SP  - 91
EP  - 96
KW  - 
UR  - https://doi.org/10.1071/C96136 
N2  - 2-Aryl-3-methoxy-6-(pyridinylmethylthio and pyridinylmethylamino)imidazo&#91;1,2-b&#93;pyridazines have been prepared and examined as ligands for benzodiazepine receptors. Most were highly effective in displacing &#91;3H&#93;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&#8242;,4&#8242;-methylenedioxyphenyl)-6-(pyridin-2&#8242;&#8242;-ylmethylthio)imidazo&#91;1,2-b&#93;pyridazine had an IC50 value of 1 &#183; 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&#8242;-methoxybenzylamino)-2-(3&#8242;&#8242;,4&#8242;&#8242;-methylenedioxyphenyl)imidazo&#91;1,2-b&#93;pyridazine was the most active in displacing &#91;3H&#93;diazepam from central receptors (IC50 0&#183;3 nM), and it had a low affinity for mitochondrial receptors (40% displacement of &#91;3H&#93;diazepam at 1000 nM). 
ER  -

