Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
|
pubmed:dateCreated |
1985-10-17
|
pubmed:abstractText |
A series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines were synthesized and tested for their ability to inhibit the binding of [3H]diazepam to rat brain receptors in vitro. Compounds bearing a phenyl, 4-methoxyphenyl, or methyl group at position 3 and a dialkylamino group at position 6 showed the highest affinity in the binding assay and were subsequently evaluated for their anticonflict and anticonvulsant effects. All of these compounds (5a-1 and 5q) were active in the Vogel rat conflict procedure, but none prevented convulsions in mice induced either by metrazol or bicuculline. 3-Phenyl-6-pyrrolidinylpyridazino[4,3-c]isoquinoline (5d) with a Ki = 11.4 nM in the binding assay exhibited the best potency in the anticonflict assay (MED 5 mg/kg ip) and did not produce neuromuscular impairment at the highest dose tested (50 mg/kg ip).
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
28
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1314-9
|
pubmed:dateRevised |
2008-11-21
|
pubmed:meshHeading |
pubmed-meshheading:2993620-Animals,
pubmed-meshheading:2993620-Binding, Competitive,
pubmed-meshheading:2993620-Chemical Phenomena,
pubmed-meshheading:2993620-Chemistry,
pubmed-meshheading:2993620-Conflict (Psychology),
pubmed-meshheading:2993620-Diazepam,
pubmed-meshheading:2993620-Isoquinolines,
pubmed-meshheading:2993620-Male,
pubmed-meshheading:2993620-Mice,
pubmed-meshheading:2993620-Pyridazines,
pubmed-meshheading:2993620-Rats,
pubmed-meshheading:2993620-Rats, Inbred Strains,
pubmed-meshheading:2993620-Receptors, GABA-A,
pubmed-meshheading:2993620-Seizures,
pubmed-meshheading:2993620-Structure-Activity Relationship
|
pubmed:year |
1985
|
pubmed:articleTitle |
Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties.
|
pubmed:publicationType |
Journal Article,
Comparative Study
|