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Arzneimittelforschung 2007; 57(9): 562-567
DOI: 10.1055/s-0031-1296650
Local Anaesthetics
Editio Cantor Verlag Aulendorf (Germany)

A Synopsis on Different Homologous Series of Fomocaine Derivatives

Amelie Lupp
1   Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany
,
Elke Karge
1   Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany
,
Thomas Dahse
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Peter Glassl
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Beate Jung
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Monika Listing
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Andreas Seeling
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Johannes Wange
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Janett Wennek-Klose
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Herbert Oelschläger
2   Institute of Pharmacy, Friedrich Schiller University, Jena, Germany
,
Christian Fleck
1   Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany
› Author Affiliations
Further Information

Publication History

Publication Date:
21 December 2011 (online)

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Abstract

Fomocaine (CAS 56583-43-6) is a basic ether-type local anaesthetic used in der-matological practice for surface anaesthesia. For many years, modifications of the fomocaine molecule have been pursued, e.g. to improve its physicochemical properties and also in view of possible new (systemic) applications, e.g. in the treatment of migraine or as antiarrhyth-mic.

The present paper provides a survey of the investigations undertaken with all the different series of fomocaine derivatives synthesized so far with respect to their in vitro interaction capacity at the cyto-chrome P450 system, in vivo toxicity (LD50; paresis of the N. ischiadicus) and local anaesthetic effects (conduction anaesthesia at the N. ischiadicus; surface anaesthesia of the cornea) in rats. The main objective of this systematic comparison of the effects of all these substances was to assess possible basic structure-activity relationships.

Key words

CAS 56583-43-6 - Cytochrome P450 - Fomocaine, derivatives, rat, toxicity - Local anaesthetics