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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
|
| pubmed:dateCreated |
1989-4-6
|
| pubmed:abstractText |
The putative behavioral effects of the enantiomers of BAY K 8644 and the behavioral responses to (+/-)-BAY K 8644 following chronic injection were assessed on motor function in mice. The interaction of the enantiomers of BAY K 8644 with mouse brain dihydropyridine binding sites was also evaluated. The calcium channel activating enantiomer (-)-S-BAY K 8644 impaired rotarod and motor activity with an ED50 value of 0.5 mg/kg. The calcium channel blocker enantiomer (+)-R-BAY K 8644 neither affected rotarod nor motor activity. (+)-R-BAY K 8644, and the structurally related dihydropyridine calcium channel blockers nifedipine and (-)-202-791 inhibited the impairment of rotarod activity by (-)-S-BAY K 8644 in a dose-dependent manner. (+/-)-BAY K 8644 produced convulsions in mice with a CD50 of 5 mg/kg. Chronic injection of (+/-)-BAY K 8644 (8 mg/kg IP once each day for four days) resulted in a significant tolerance to, and increase in recovery from, the motor deficits produced by (+/-)-BAY K 8644. Furthermore, chronic treatment with (+/-)-BAY K 8644 increased the onset time, but did not reduce the number of mice having convulsions to (+/-)-BAY K 8644. Chronic injection of nifedipine did not affect the motor deficit and convulsive activity of (+/-)-BAY K 8644. The behavioral effects of (+/-)-BAY K 8644 were observed at significant brain levels of drug. [3H]Nitrendipine binding to mouse brain dihydropyridine binding sites was unchanged in mice chronically injected with either (+/-)-BAY K 8644 or nifedipine.(ABSTRACT TRUNCATED AT 250 WORDS)
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Dec
|
| pubmed:issn |
0361-9230
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
21
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
865-72
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:2465070-3-Pyridinecarboxylic acid...,
pubmed-meshheading:2465070-Animals,
pubmed-meshheading:2465070-Binding, Competitive,
pubmed-meshheading:2465070-Brain,
pubmed-meshheading:2465070-Calcium Channels,
pubmed-meshheading:2465070-Dose-Response Relationship, Drug,
pubmed-meshheading:2465070-Drug Tolerance,
pubmed-meshheading:2465070-Injections, Intraperitoneal,
pubmed-meshheading:2465070-Male,
pubmed-meshheading:2465070-Mice,
pubmed-meshheading:2465070-Motor Activity,
pubmed-meshheading:2465070-Nifedipine,
pubmed-meshheading:2465070-Stereoisomerism
|
| pubmed:year |
1988
|
| pubmed:articleTitle |
Enantiomer selectivity and the development of tolerance to the behavioral effects of the calcium channel activator BAY K 8644.
|
| pubmed:affiliation |
Division of Basic Medical Sciences, Faculty of Medicine, Memorial University of Newfoundland, St. John's, Canada.
|
| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|