[General pharmacology of 6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. II. Effects on the peripheral system (author's transl)].
The general pharmacology of afloqualone, a new centrally acting muscle relaxant, in the peripheral system, was examined in laboratory animals and findings compared with those of some other central muscle relaxants. Afloqualone dose dependently inhibited respiration, lowered arterial blood pressure, decreased heart rate, and slightly increased femoral and renal arterial blood flow in parallel with hypotension, at doses of 1 or 2 to 20 mg/kg iv. in anesthetized cats. Afloqualone also inhibited cardiac movement in situ in anesthetized rabbits and decreased internal pressure in the urinary bladder in anesthetized cats. In in vitro experiments, afloqualone inhibited spontaneous movements of isolated rabbit atrium and ileum and isolated rat uterus at considerably high concentrations of 10(-6) g/ml or more. Oral administration of afloqualone, however, had no significant influence on respiration, the cardiovascular, digestive, and autonomic nervous systems, and urogenital organs, at doses up to 50 mg/kg except for a comparatively potent inhibitory effect on carrageenin-induced paw edema in rats. Afloqualone induced neither surface nor infiltration anesthesia.
D000818:Animals; D000893:Anti-Inflammatory Agents; D001341:Autonomic Nervous System / Q000187:drug effects; D002319:Cardiovascular System / Q000187:drug effects; D002415:Cats; D004064:Digestive System / Q000187:drug effects; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009125:Muscle Relaxants, Central / Q000494:pharmacology*; D011247:Pregnancy; D011799:Quinazolines / Q000008:administration & dosage / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012119:Respiration / Q000187:drug effects; D014566:Urogenital System / Q000187:drug effects; D014590:Uterine Contraction / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D009125:Muscle Relaxants, Central; D011799:Quinazolines; C033541:afloqualone