Selected cardiovascular and central properties of three lidocaine analogs.
Three analogs of lidocaine (benzyl carbamyl, benzyl nitrile and methyl nitrile) were synthesized and examined for cardiovascular and central activity. The benzyl carbamyl analog was more potent than lidocaine in lowering blood pressure but possessed only slight local anesthetic, antiarrhythmic and CNS-depressant activity. At 40 mg/kg the benzyl nitrile derivative was superior to lidocaine in protecting against chloroform-induced arrhythmias. The methyl nitrile analog was less active than the benzyl nitrile analog in most parameters examined. The benzyl nitrile derivative and lidocaine had similar potencies on blood pressure depression, local anesthetic activity and ability to protect against calcium chloride-induced arrhythmias. Unlike the benzyl carbamyl derivative both lidocaine and the benzyl nitrile compounds appear to depress the cardiovascular system via a common mechanism.
D000779:Anesthetics, Local; D000818:Animals; D000889:Anti-Arrhythmia Agents; D001794:Blood Pressure / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects*; D008012:Lidocaine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D012119:Respiration / Q000187:drug effects
D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D008012:Lidocaine