General pharmacology of the new antitussive levodropropizine.
The general pharmacological profile of levodropropizine (S(-)3-(4-phenyl-piperazin-1-yl)-propane-1,2-diol, DF 526), a new antitussive drug, was compared with that of dropropizine racemate. Levodropropizine had weaker central sedative effects than the racemate and it did not induce physical dependence in rats. When given intravenously or intraperitoneally, levodropropizine did not exert any significant effects on the cardiovascular and respiratory systems. Receptor binding data excluded interaction with beta-adrenergic, muscarinic and opiate receptors. On the contrary, levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors. The affinity was also confirmed with isolated organ preparations. On the basis of this study, levodropropizine appears to have a better tolerability index than the racemate.
Melillo
G
G
Research & Development Laboratories, Dompé Farmaceutici S.p.A., Milan, Italy.
Malandrino
S
S
Rossoni
G
G
Caselli
G
G
Bestetti
A
A
Borsa
M
M
Tonon
G C
GC
Berti
F
F
D000403:Airway Resistance / Q000187:drug effects; D000818:Animals; D000996:Antitussive Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000187:drug effects; D002415:Cats; D004064:Digestive System / Q000187:drug effects; D004285:Dogs; D004562:Electrocardiography; D004569:Electroencephalography; D005260:Female; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D051379:Mice; D009420:Nervous System / Q000187:drug effects; D011409:Propylene Glycols / Q000008:administration & dosage / Q000494:pharmacology*; D011817:Rabbits; D011897:Random Allocation; D051381:Rats; D012119:Respiration / Q000187:drug effects; D012890:Sleep / Q000187:drug effects
D000996:Antitussive Agents; D011409:Propylene Glycols; C035916:dipropizine