Paradoxical reversion of the inhibitory effects of dihydropyridine enantiomers on the calcium current in frog heart by CGP 28861

A dihydropyridine CGP 28861 (5 × 10−6m) did not change slow inward Ca current as measured by the double sucrose gap method in frog atrial fibres but decreased the agonist effects of Bay K 8644, CGP 28392, (+m)−(S)−202–791 and the antagonist effects of nifedipine and (+m)−(PN)−200–110. Paradoxically,...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	British journal of pharmacology 1989-02, Vol.96 (2), p.253-255
Hauptverfasser:	Filippov, Alexander, Kobrinsky, Evgeny, Porotikov, Vladimir, Saxon, Maya
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester - pharmacology Animals Biological and medical sciences Calcium Channels Cardiovascular system Drug Interactions Female Heart Atria - drug effects In Vitro Techniques Male Medical sciences Membrane Potentials - drug effects Miscellaneous Pharmacology. Drug treatments Pyridines - pharmacology Rana ridibunda Receptors, Nicotinic - drug effects
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A dihydropyridine CGP 28861 (5 × 10−6m) did not change slow inward Ca current as measured by the double sucrose gap method in frog atrial fibres but decreased the agonist effects of Bay K 8644, CGP 28392, (+m)−(S)−202–791 and the antagonist effects of nifedipine and (+m)−(PN)−200–110. Paradoxically, the weak antagonists (−)−(R)−202–791, (−)−(PN)−200–110 and (+)‐Bay K 8644 increased Ca‐current after washout of CGP 28861. These data suggest that CGP 28861 can convert the dihydropyridine Ca‐channel receptor from an antagonistic site into an agonistic one.
ISSN:	0007-1188 1476-5381
DOI:	10.1111/j.1476-5381.1989.tb11808.x