Study of local anaesthetics. Part 98(3): Preparation and local anaesthetic activity of 4-alkylpiperazinoethyl esters of o-heptyloxyphenylcarbamic acid.
During the course of study of variations in the basic moiety of heptacainium chloride 10 derivatives of 4-alkylpiperazinoethyl esters of o-heptyloxyphenylcarbamic acid were prepared. Pharmacological investigation indicated that practically all the new compounds were several times more active than standards (cocaine and procaine). The most effective compound was 1-[2-(o-heptyloxyphenylcarbamoyloxy)ethyl]-4-butyl-piperazinium dichloride, which was 142 times more active than cocaine and 266 times more active than procaine.
Minh
D N
DN
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Bratislava, CSFR.
Cizmárik
J
J
Medvecký
R
R
Racanská
E
E
D000779:Anesthetics, Local / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002219:Carbamates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D003042:Cocaine / Q000494:pharmacology; D006168:Guinea Pigs; D007928:Lethal Dose 50; D051379:Mice; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011343:Procaine / Q000494:pharmacology
D000779:Anesthetics, Local; D002219:Carbamates; D010879:Piperazines; D010880:Piperidines; D011343:Procaine; C013549:heptacaine; D003042:Cocaine