A synopsis on different homologous series of fomocaine derivatives. In vitro interactions with the cytochrome P450 system, toxicity, and local anaesthetic effects in rats--Part 1.

Abstract	Fomocaine (CAS 56583-43-6) is a basic ether-type local anaesthetic used in dermatological 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 antiarrhythmic. 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 cytochrome 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.
Authors	Amelie Lupp, Elke Karge, Thomas Dahse, Peter Glassl, Beate Jung, Monika Listing, Andreas Seeling, Johannes Wange, Janett Wennek-Klose, Herbert Oelschläger, Christian Fleck
Journal	Arzneimittel-Forschung (Arzneimittelforschung) Vol. 57 Issue 9 Pg. 562-7 ( 2007) ISSN: 0004-4172 [Print] Germany
PMID	17966754 (Publication Type: Journal Article)
Chemical References	Anesthetics, Local Phenyl Ethers Tetracaine fomocain Procaine Cytochrome P-450 Enzyme System Cytochrome P-450 CYP1A1
Topics	Anesthetics, Local (chemistry, pharmacology, toxicity) Animals Chemical Phenomena Chemistry, Physical Cornea (drug effects) Cytochrome P-450 CYP1A1 (metabolism) Cytochrome P-450 Enzyme System (chemistry) Female Lethal Dose 50 Luminescence Male Microsomes, Liver (drug effects, metabolism) Neural Conduction (drug effects) Neutrophils (physiology) Paralysis (chemically induced) Phenyl Ethers (chemistry, pharmacology, toxicity) Procaine (pharmacology) Rats Rats, Wistar Structure-Activity Relationship Tetracaine (pharmacology)

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