Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
|
pubmed:dateCreated |
1991-12-13
|
pubmed:abstractText |
The effects of (S)-nafenodone, a new antidepressant, on transmembrane action potentials were studied in guinea-pig papillary muscles. In muscles driven at 0.02 and 1 Hz, (S)-nafenodone, 10(-6) mol/l and 10(-5) mol/l, produced a concentration-dependent decrease in the maximum upstroke velocity of the action potential, but it had no effect of the resting membrane potential. In the presence of 10(-5) mol/l (S)-nafenodone, trains of stimuli at rates between 0.5 and 2 Hz led to an exponential decline in maximum upstroke velocity to a new steady-state level [K = 0.152 +/- 0.03 (action potential)-1 at 2 Hz]. This frequency-dependent maximum upstroke velocity block increased at higher stimulation frequencies and at higher drug concentrations. (S)-Nafenodone also prolonged the time constant of recovery of maximum upstroke velocity from the frequency-dependent block to 2.3 +/- 0.6 s, this value being independent of the drug concentration. These values of onset and offset kinetics of (S)-nafenodone lie between those of drugs with fast and intermediate kinetic properties. (S)-nafenodone also shifted the curve relating membrane potential and maximum upstroke velocity in hyperpolarizing direction. All these results indicated that (S)-nafenodone produced a frequency- and voltage-dependent inhibition of the fast sodium channels similar to that exhibited with imipramine.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0028-1298
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
343
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
638-44
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:1944605-Action Potentials,
pubmed-meshheading:1944605-Animals,
pubmed-meshheading:1944605-Antidepressive Agents,
pubmed-meshheading:1944605-Biological Transport, Active,
pubmed-meshheading:1944605-Dose-Response Relationship, Drug,
pubmed-meshheading:1944605-Electric Stimulation,
pubmed-meshheading:1944605-Female,
pubmed-meshheading:1944605-Guinea Pigs,
pubmed-meshheading:1944605-Male,
pubmed-meshheading:1944605-Membrane Potentials,
pubmed-meshheading:1944605-Myocardial Contraction,
pubmed-meshheading:1944605-Naphthalenes,
pubmed-meshheading:1944605-Papillary Muscles,
pubmed-meshheading:1944605-Sodium
|
pubmed:year |
1991
|
pubmed:articleTitle |
Tonic and frequency-dependent Vmax block induced by (S)-nafenodone, a new antidepressant drug, in guinea-pig papillary muscles.
|
pubmed:affiliation |
Department of Pharmacology, School of Medicine, Universidad Complutense, Madrid, Spain.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|