The electrophysiologic effects of ORG 30701 (1-8 x 10(-6) M) were tested in a thin, two-dimensional sheet of ventricular myocardium. Special attention was paid to a possible promotion of reentrant excitation. The drug did not increase the degree of inhomogeneity of conduction and because of the marked effect on refractoriness prevent fast rates (either spontaneously or driven). If the extracellular potassium concentration was lowered (from 5.6 to 2.0 mM), the enhancement of refractoriness by the drug was more marked. The changes in refractoriness do not appear to be based on lengthening of the repolarization of the action potential, but rather on post-repolarization refractoriness; therefore, the occurrence of triggered activity (early afterdepolarizations) is not anticipated. ORG 30701 is a cardioactive drug that because of its calcium antagonistic action acts as an antianginal drug and, in addition, exhibits antiarrhythmic properties.

01 Aug 1992·British Journal of PharmacologyQ2 · MEDICINE

Mode of action and comparative efficacy of pharmacological agents that inhibit calcium‐dependent dehydration of sickle cells

Q2 · MEDICINE

Article

Author: E. Horwitz ; J. Stuart ; J.C. Ellory ; G.B. Nash ; P.C.W. Stone ; S.J. Culliford

1. Selected Ca-channel antagonists were tested at 20 microM as inhibitors of Ca(2+)-uptake in human sickle red cells. Nitrendipine, fendiline, and bepridil (and its stereoisomers), were found to be as effective as methoxyverapamil (D-600) in inhibiting a fraction (25%) of Ca(2+)-uptake. In contrast cetiedil and Org 30701 were ineffective. 2. The drugs were subsequently tested as inhibitors of Ca(2+)-induced K+ efflux (Gardos) from sickle cells. They all showed inhibitory activity, with the order of efficacy nitrendipine greater than fendiline greater than bepridil greater than cetiedil greater than Org 30701. 3. With a 15 h programme of deoxygenation/reoxygenation cycles in a gas exchanger, it was shown that the inhibitors protected against cellular dehydration and loss of filterability in the order nitrendipine greater than fendiline greater than bepridil greater than cetiedil greater than Org 30701. However, significant stomatocytosis occurred at high concentrations of cetiedil, and bepridil (including its stereoisomers and analogues) impairing cell deformability. 4. It is concluded that Ca-antagonists may partially block both Ca(2+)-uptake and Ca(2+)-induced K+ efflux. The latter pathway is significant in contributing to sickle cell dehydration and nitrendipine is the most effective inhibitor of this route.

01 Sep 1990·The American Journal of CardiologyQ3 · MEDICINE

Effects of bepridil and CERM 4205 (ORG 30701) on the relation between cardiac cycle length and QT duration in healthy volunteers

Q3 · MEDICINE

Article

Author: Pierre-Louis Prost ; Vincent Lecocq ; Pierre Boisson ; Patrice Jaillon ; Brigitte Lecocq ; Odile Fleurot

Bepridil is a calcium antagonist that prolongs the duration of ventricular repolarization, whereas CERM 4205, another calcium antagonist, seems to be devoid of any effect on QT interval. The aim of this study was to compare the effects of bepridil and CERM 4205 on the QT-RR relation at different heart rates during rest and exercise and the results of pharmacologic tests designed to vary neurovegetative tone. Twelve healthy men (21 to 37 years) participated in a placebo-controlled, randomized, crossover, double-blind study and received either bepridil (200 mg/day twice daily) or CERM 4205 (200 mg/day twice daily), or matching placebo during three 14-day treatment periods at 2-week intervals. Bepridil, but not CERM 4205, caused a significant prolongation of resting QT interval. The RR-QT relation was monoexponential for all subjects during resting and exercising physiologic conditions and remained unchanged after 14 days with placebo or CERM 4205. Bepridil significantly shifted the relation upward, resulting in a rate-dependent QT prolongation that predominated during bradycardia. After isoprenaline, QT no longer adapted to changes in heart rate, whereas atropine resulted in a rate-dependent shortening in QT. These results suggest that bepridil and CERM 4205 exert different effects on ventricular repolarization, since only bepridil significantly prolonged QT duration. Bepridil-induced prolongation of QT increased at slow heart rates, which could explain the greater incidence of torsades de pointes in bradycardia.

100 Deals associated with Dopropidil Hydrochloride

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Angina Pectoris	Phase 2	FR	Akzo Nobel NV	-
Arrhythmias, Cardiac	Phase 2	FR	Akzo Nobel NV	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Dopropidil Hydrochloride

Overview

Basic Info

Structure

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation