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Sandermann, H.

Ecotoxicology of narcosis: Stereoselectivity and potential target sites.

Chemosphere 72, 1256-1259 (2008)
DOI
Open Access Gold möglich sobald Verlagsversion bei der ZB eingereicht worden ist.
The stereoselectivity of certain anesthetics is currently thought to be inconsistent with lipid theories of narcosis. The EC(50)-values of etomidate enantiomers for tadpole narcosis are now examined as a function of octanol/water partition coefficients, and enhancement factors for predicted over experimental EC(50) values are determined from a calibration curve for non-selective narcosis. The unfavored S-(-)-enantiomers of etomidate and two analogues surprisingly still fulfill the Meyer-Overton rule. The R(+)-enantiomers of etomidate and four structural analogues are up to 34-fold more active than expected. The non-chiral anesthetic, propofol, is 8-fold more active than expected. It is concluded that there may be two pathways to tadpole narcosis: enhanced narcosis involving specific receptor binding sites and non-selective narcosis corresponding to the Meyer-Overton rule and operating on the lipid/protein interface.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Schlagwörter Tadpole narcosis; Stereoselectivity; Etomidate; Propofol; GABAA channel; Lipid/protein interface
ISSN (print) / ISBN 0045-6535
e-ISSN 1879-1298
Zeitschrift Chemosphere
Quellenangaben Band: 72, Heft: 9, Seiten: 1256-1259 Artikelnummer: , Supplement: ,
Verlag Elsevier
Verlagsort Kidlington, Oxford
Begutachtungsstatus Peer reviewed
Institut(e) Institute of Biochemical Plant Pathology (BIOP)