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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1990-7-31
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pubmed:abstractText |
The behavioral (deficits in motor function in mice), neurochemical (affinity for mouse brain membrane dihydropyridine receptors, effects on neurotransmitter/metabolite levels in mice) and pharmacologic (effect on the contractile activity of guinea pig ileal longitudinal smooth muscle) properties of the calcium channel activators (+/-)-BAY K 8644, (+/-)-202-791 (and their corresponding channel activating and antagonist enantiomers) and CGP-28392 were investigated and compared. The calcium channel activating enantiomers (-)-S-BAY K 8644, (+)-S-202-791 and (+/-)-BAY K 8644, (+/-)-202-791 and CGP-28392 produced a dose-dependent impairment of rotarod ability and decreases in motor activity in mice with the following order of potency: (-)-S-BAY K 8644 greater than (+/-)-BAY K 8644 much greater than (+)-S-202-791 greater than (+/-)-202-791 = CGP-28392. The calcium channel antagonists (+)-R-BAY K 8644 and (-)-R-202-791 were behaviorally inactive but blocked the behavioral effects of (-)-S-BAY K 8644. The binding of dihydropyridine calcium channel activator and antagonist enantiomers to mouse brain membranes was described by both one and two site models. (-)-S-BAY K 8644, (+/-)-BAY K 8644, (+)-S-202-791 and CGP-28392 produced contractions in partially depolarized (15 mM K+) strips of guinea pig ileal longitudinal smooth muscle which differed in the degree of maximum contraction obtained. (+)-R-BAY K 8644 and (-)-R-202-791 inhibited potassium-induced contractions (80 mM K+) in guinea pig ileal longitudinal smooth muscle.(ABSTRACT TRUNCATED AT 250 WORDS)
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/3-Pyridinecarboxylic acid...,
http://linkedlifedata.com/resource/pubmed/chemical/CGP 28392,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Catecholamines,
http://linkedlifedata.com/resource/pubmed/chemical/Dihydropyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotinic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Nifedipine,
http://linkedlifedata.com/resource/pubmed/chemical/Oxadiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/PN 202-791,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-3565
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
253
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
905-12
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1694243-3-Pyridinecarboxylic acid...,
pubmed-meshheading:1694243-Animals,
pubmed-meshheading:1694243-Brain,
pubmed-meshheading:1694243-Calcium Channel Agonists,
pubmed-meshheading:1694243-Catecholamines,
pubmed-meshheading:1694243-Chromatography, High Pressure Liquid,
pubmed-meshheading:1694243-Dihydropyridines,
pubmed-meshheading:1694243-Guinea Pigs,
pubmed-meshheading:1694243-Injections, Intraperitoneal,
pubmed-meshheading:1694243-Male,
pubmed-meshheading:1694243-Mice,
pubmed-meshheading:1694243-Motor Activity,
pubmed-meshheading:1694243-Muscle, Smooth,
pubmed-meshheading:1694243-Muscle Contraction,
pubmed-meshheading:1694243-Nicotinic Acids,
pubmed-meshheading:1694243-Nifedipine,
pubmed-meshheading:1694243-Oxadiazoles,
pubmed-meshheading:1694243-Pyridines,
pubmed-meshheading:1694243-Stereoisomerism,
pubmed-meshheading:1694243-Structure-Activity Relationship
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pubmed:year |
1990
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pubmed:articleTitle |
Comparative behavioral, neurochemical and pharmacological activities of dihydropyridine calcium channel activating drugs.
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pubmed:affiliation |
Division of Basic Medical Sciences, Faculty of Medicine, Memorial University of Newfoundland, St. John's, Canada.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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