The effects on cardiac muscle and nerve of a fluorinated decahydroquinoline derivative, L7810, rapidly absorbed after oral administration.
1. L7810 (4-carbamoyloxy-1-(4-(4-fluorophenyl)-4-oxobutyl) decahydroquinoline, has a local anaesthetic action on frog nerve 1.75 times that of procaine.2. L7810 protected anaesthetized guinea-pigs against ouabain-induced ventricular fibrillation and increased the lethal dose of ouabain.3. L7810 reduced the rate of rise of intracellularly recorded action potentials in rabbit isolated atria; the resting potential was not affected, but the duration of the action potential was prolonged.4. Unlike most drugs with local anaesthetic properties L7810 did not depress contractions in isolated atria but increased them.5. L7810 reduced the spontaneous frequency, maximum follow frequency and conduction velocity of rabbit isolated atria.6. L7810 had no blocking action on the chronotropic or positive inotropic actions of isoprenaline on isolated atrial muscle.7. In anaesthetized dogs L7810 caused a small dose-related bradycardia, and a large dose-related decrease in peripheral vascular resistance. There was no blockade of the effects of isoprenaline on heart rate or peripheral blood flow.
D000200:Action Potentials / Q000187:drug effects; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000779:Anesthetics, Local / Q000494:pharmacology; D000818:Animals; D001001:Anura; D001145:Arrhythmias, Cardiac / Q000139:chemically induced; D001775:Blood Circulation / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D002219:Carbamates / Q000494:pharmacology; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects*; D006325:Heart Atria / Q000187:drug effects; D006329:Heart Conduction System / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology; D009132:Muscles / Q000187:drug effects*; D010042:Ouabain / Q000037:antagonists & inhibitors; D011804:Quinolines / Q000494:pharmacology*; D012584:Sciatic Nerve / Q000187:drug effects; D013997:Time Factors; D014655:Vascular Resistance / Q000187:drug effects
D000319:Adrenergic beta-Antagonists; D000779:Anesthetics, Local; D002219:Carbamates; D011804:Quinolines; D010042:Ouabain; D007545:Isoproterenol