Biomaterial Database

[Local anesthetics. CX. Preparation, activity and partition coefficients of pyrrolidinoethylesters of 2-, 3- and 4-alkoxy-substituted phenylcarbamic acids]. 1993

J Cizmárik, and E Polásek, and P Svec, and E Racanská

Katedra farmaceutickej chémie Farmaceutickej fakulty Univerzity Komenského, Bratislava.

By pyrrolidinoethylalcohol addition on 2-, 3- and 4-alkoxy-substituted phenylisocyanate in non-aqueous toluene medium a series of 30 compounds of the type Pyrrolidinoethylesters of 2-, 3- and 4-alkoxy substituted phenylcarmabim acids were prepared. Pharmacological evaluation results shown after comparing with cocaine and procaine standards that these compounds have a higher index of effectiveness in both types of local anaesthesia. The maximum effectiveness of surface anaesthesia shows Pyrrolidinoethylester of 2-octyloxy phenylcarbamic acid which is 204-times more effective as cocaine. The maximum effectiveness of infiltration anaesthesis shows Pyrrolidinoethylester of 2-heptyloxy phenylcarbamic acid which is 66-times more effective as procaine. Prepared compounds are more effective in the case of surface anaesthesia as in the case of infiltration anaesthesia and they have comparatively high values of partition coefficients P' and P' cal. Comparison of prepared compounds effectiveness and analogic piperidinoethylesters shows that in more cases they are either equal or nearer effective. The values of their P' and P' cal correlate with these results.

UI	MeSH Term	Description	Entries
D011759	Pyrrolidines	Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH.	Tetrahydropyridine,Tetrahydropyridines
D002219	Carbamates	Derivatives of carbamic acid, H2NC(	Carbamate,Aminoformic Acids,Carbamic Acids,Acids, Aminoformic,Acids, Carbamic
D000779	Anesthetics, Local	Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate.	Anesthetics, Conduction-Blocking,Conduction-Blocking Anesthetics,Local Anesthetic,Anesthetics, Topical,Anesthetic, Local,Anesthetics, Conduction Blocking,Conduction Blocking Anesthetics,Local Anesthetics,Topical Anesthetics
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D051379	Mice	The common name for the genus Mus.	Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus