m-Azipropofol (AziPm) a photoactive analogue of the intravenous general anesthetic propofol.
Publication/Presentation Date
8-12-2010
Abstract
Propofol is the most commonly used sedative-hypnotic drug for noxious procedures, yet the molecular targets underlying either its beneficial or toxic effects remain uncertain. In order to determine targets and thereby mechanisms of propofol, we have synthesized a photoactivateable analogue by substituting an alkyldiazirinyl moiety for one of the isopropyl arms but in the meta position. m-Azipropofol retains the physical, biochemical, GABA(A) receptor modulatory, and in vivo activity of propofol and photoadducts to amino acid residues in known propofol binding sites in natural proteins. Using either mass spectrometry or radiolabeling, this reagent may be used to reveal sites and targets that underlie the mechanism of both the desirable and undesirable actions of this important clinical compound.
Volume
53
Issue
15
First Page
5667
Last Page
5675
ISSN
1520-4804
Published In/Presented At
Hall, M. A., Xi, J., Lor, C., Dai, S., Pearce, R., Dailey, W. P., & Eckenhoff, R. G. (2010). m-Azipropofol (AziPm) a photoactive analogue of the intravenous general anesthetic propofol. Journal of medicinal chemistry, 53(15), 5667–5675. https://doi.org/10.1021/jm1004072
Disciplines
Anesthesiology | Medicine and Health Sciences
PubMedID
20597506
Department(s)
Department of Anesthesiology
Document Type
Article