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Antiarrhythmic effects of DPI 201‐106
Author(s) -
Scholtysik Günter,
Williams Frances M.
Publication year - 1986
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1986.tb10258.x
Subject(s) - medicine , pharmacology , chemistry
1 The cardiotonic agent DPI 201‐106 (4‐[3‐(4‐diphenylmethyl‐1‐piperazinyl‐2‐hydroxypropyl]‐1H‐ indole‐2‐carbonitrile) which modifies the sarcolemmal Na + channel gating system and has electrophysiological properties of class III antiarrhythmics was investigated for local anaesthetic and antiarrhythmic activity. 2 The compound action potential amplitude of cat cervical vagus nerves in vitro was decreased by DPI 201‐106 in a concentration‐dependent manner, the IC 50 being 1.82 × 10 −5 M. This was paralleled by a slowing in conduction velocity and demonstrates local anaesthetic effects. 3 Ventricular fibrillation which occurs in response to coronary artery reperfusion in rats was prevented by intravenous infusions of 0.3 mg kg −1 min −1 of DPI 201‐106. 4 The arrhythmogenic intravenous doses of aconitine in rats were increased following pretreatment with DPI 201‐106 in a dose‐dependent manner. 5 DPI 201‐106 did not protect against ouabain‐induced arrhythmias in guinea‐pigs. 6 The results demonstrate that DPI 201‐106 has local anaesthetic effects and is a potential antiarrhythmic.