[Preparation and pharmacologic characteristics of aryloxyaminopropanol derivatives with an assumed cardiovascular effect].
In an attempt to prepare drugs favourably influencing pathologically changed functions of the cardiovascular system, such as hypertension and ischemic cardiac disease, several chemical compounds were prepared in which benzhydrylpiperazine, alkyl, or substituted phenylpiperazine (fragments of the structures of calcium antagonists) were bound to the fundamental aryloxyamino-propanol skeleton (the carrier of beta-adrenolytic effect). The selected four compounds underwent basic pharmacological analysis. In experiments on the isolated spontaneously beating guinea-pig atria (beta 1), three compounds competitively inhibited the positively chronotropic effect of isoprenaline (pA2 = 6.40-7.24) and in experiments on the isolated tracheal guinea-pig muscle they antagonised the relaxation effect of isoprenaline beta 2, the pA2 values ranging from 5.90-7.58. It follows from the experiments on the isolated guinea-pig aorta contracted with 50 mM KCl that all compounds under study possess mild relaxation effects, the intensity of which is, however, lower than in the used standards flunarizine and verapamil.
Mlynárová
R
R
Katedra farmakológie a toxikológie Farmaceutickej fakulty Univerzity Komenského, Bratislava.
Celková
H
H
Racanská
E
E
D000433:1-Propanol / Q000138:chemical synthesis / Q000494:pharmacology*; D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001011:Aorta / Q000187:drug effects; D002317:Cardiovascular Agents / Q000494:pharmacology*; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D020005:Propanols; D051381:Rats; D017208:Rats, Wistar; D014132:Trachea / Q000187:drug effects
D000588:Amines; D002317:Cardiovascular Agents; D020005:Propanols; D000433:1-Propanol