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rdf:type |
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lifeskim:mentions |
|
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pubmed:issue |
7
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pubmed:dateCreated |
1989-10-26
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pubmed:abstractText |
The effects of new 4-aminopyridine (4-AP) derivatives were investigated in the isolated mouse phrenic nerve-hemidiaphragm preparation under single impulse stimulation and tetanic conditions. The basic 4-AP structure was modified in position 3 on the pyridine nucleus by introducing different substituents. Results were compared to those obtained with 4-AP and 3,4-diaminopyridine. The compounds were tested for their antagonistic effect against calcium antagonists and botulinum toxin A. The effect on smooth muscle was investigated on the isolated guinea-pig ileum. Physico-chemical parameters of the test compounds were determined by the partition coefficient and ionization constant. Finally structure-activity relationship analysis revealed that the activity was highly related to lipophilicity and the steric volume. So far 4-AP itself provided the most advantageous molecular structure.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0004-4172
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pubmed:author |
|
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pubmed:issnType |
Print
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pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
762-5
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:2551304-Aminopyridines,
pubmed-meshheading:2551304-Animals,
pubmed-meshheading:2551304-Botulinum Toxins,
pubmed-meshheading:2551304-Chemistry, Physical,
pubmed-meshheading:2551304-Dantrolene,
pubmed-meshheading:2551304-Guinea Pigs,
pubmed-meshheading:2551304-Ileum,
pubmed-meshheading:2551304-Male,
pubmed-meshheading:2551304-Mice,
pubmed-meshheading:2551304-Mice, Inbred ICR,
pubmed-meshheading:2551304-Muscle, Smooth,
pubmed-meshheading:2551304-Muscle Contraction,
pubmed-meshheading:2551304-Neuromuscular Junction,
pubmed-meshheading:2551304-Phrenic Nerve,
pubmed-meshheading:2551304-Physicochemical Phenomena,
pubmed-meshheading:2551304-Respiratory Muscles,
pubmed-meshheading:2551304-Synaptic Transmission,
pubmed-meshheading:2551304-Trifluoperazine,
pubmed-meshheading:2551304-Verapamil
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pubmed:year |
1989
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pubmed:articleTitle |
Effects of new 4-aminopyridine derivatives on neuromuscular transmission and on smooth muscle contractility.
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pubmed:affiliation |
Institute of Pharmacology, University of Zurich, Switzerland.
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pubmed:publicationType |
Journal Article,
In Vitro
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