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Ecotoxicology of narcosis: Stereoselectivity and potential target sites.
Chemosphere 72, 1256-1259 (2008)
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.
Impact Factor
Scopus SNIP
Web of Science
Times Cited
Times Cited
Scopus
Cited By
Cited By
Altmetric
2.739
1.880
4
7
Anmerkungen
Besondere Publikation
Auf Hompepage verbergern
Publikationstyp
Artikel: Journalartikel
Dokumenttyp
Wissenschaftlicher Artikel
Schlagwörter
Tadpole narcosis; Stereoselectivity; Etomidate; Propofol; GABAA channel; Lipid/protein interface
Sprache
englisch
Veröffentlichungsjahr
2008
HGF-Berichtsjahr
2008
ISSN (print) / ISBN
0045-6535
e-ISSN
1879-1298
Zeitschrift
Chemosphere
Quellenangaben
Band: 72,
Heft: 9,
Seiten: 1256-1259
Verlag
Elsevier
Verlagsort
Kidlington, Oxford
Begutachtungsstatus
Peer reviewed
Institut(e)
Institute of Biochemical Plant Pathology (BIOP)
POF Topic(s)
30202 - Environmental Health
Forschungsfeld(er)
Environmental Sciences
PSP-Element(e)
G-504900-001
Scopus ID
46149083203
Erfassungsdatum
2008-07-23