Plasma CPU-86017 concentrations regarding suppression of ouabain-induced cardiac arrhythmias and decrease of heart rate in guinea pigs.
OBJECTIVE
To determine the effective plasma levels of CPU-86017 which could suppress the cardiac arrhythmias induced by i.v. ouabain in guinea pigs.


METHODS
The cardiac arrhythmias and the heart rate were monitored by ECG traces. Blood samples were collected to determine plasma levels using HPLC assay. TXB2 and 6-keto-PGF1 alpha were measured in plasma.


RESULTS
The plasma concentrations of CPU-86017 which were effective to suppress ventricular fibrillation (VF) and heart rate were 0.13-0.23 mg/L and 0.13-0.31 mg/L, respectively. A reduction of TXB2 levels and an elevation of 6-keto-PGF1 alpha levels were observed after CPU-86017 i.v. administration.


CONCLUSIONS
The arrhythmia-suppressing and heart rate-slowing effect of CPU-86017 followed a linear relationship with its concentrations in plasma.
Khan
H H
HH
Research Division of Pharmacology, China Pharmaceutical University, Nanjing 210009, China.
Dai
D Z
DZ
Xiao
D W
DW
Lin
S
S
Wang
Z Z
ZZ
Lou
S
S
Qing
Q
Q
D015121:6-Ketoprostaglandin F1 alpha / Q000097:blood; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000097:blood / Q000494:pharmacology*; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000188:drug therapy*; D001599:Berberine / Q000031:analogs & derivatives / Q000097:blood / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects*; D008297:Male; D010042:Ouabain; D013929:Thromboxane B2 / Q000097:blood
C400084:4-chlorobenzyltetrahydroberberine; D000889:Anti-Arrhythmia Agents; D001599:Berberine; D013929:Thromboxane B2; D015121:6-Ketoprostaglandin F1 alpha; D010042:Ouabain