The anti-ischaemic activity of the novel compound, CERM 11956, compared with that of bepridil and nifedipine in isolated guinea-pig hearts.
A comparison between the protective activity of bepridil, its novel derivative, CERM 11956, and nifedipine in isolated electrically paced guinea-pig hearts after 60 min of global ischaemia followed by 30 min of reperfusion has been made. All three compounds exerted a significant anti-ischaemic effect, as indicated by an improved recovery of functional parameters (left ventricular pressure and coronary perfusion), a delayed onset of the ischaemic contracture, and an enhanced recovery of biochemical (CrP, ATP and adenylate energy charge) parameters. The most pronounced anti-ischaemic activity was shown by the compound CERM 11956 at concentrations that displayed only minor negative inotropic activity. From the results it may be concluded that the new bepridil derivative, CERM 11956, is a promising and potent anti-ischaemic compound, which has little influence on haemodynamic parameters.
Boddeke
E W
EW
Division of Pharmacotherapy/Pharmacology, University of Amsterdam, The Netherlands.
Wilffert
B
B
Heynis
J B
JB
Hugtenburg
J G
JG
Jap
W T
WT
Veldsema-Currie
R D
RD
Van Zwieten
P A
PA
D000255:Adenosine Triphosphate / Q000494:pharmacology; D000818:Animals; D015764:Bepridil; D002121:Calcium Channel Blockers / Q000627:therapeutic use*; D003326:Coronary Circulation / Q000187:drug effects; D003327:Coronary Disease / Q000188:drug therapy*; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D009543:Nifedipine / Q000627:therapeutic use*; D010725:Phosphocreatine / Q000494:pharmacology; D011759:Pyrrolidines / Q000627:therapeutic use*
D002121:Calcium Channel Blockers; D011759:Pyrrolidines; D010725:Phosphocreatine; D015764:Bepridil; D000255:Adenosine Triphosphate; C056894:CERM 11956; D009543:Nifedipine