m-Azipropofol (AziPm) a photoactive analogue of the intravenous general anesthetic propofol.

m-Azipropofol (AziPm) a photoactive analogue of the intravenous general anesthetic propofol.
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DOI:
10.1021/jm1004072
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发表时间:
2010-08-12
影响因子:
7.3
通讯作者:
Eckenhoff RG
Eckenhoff RG
中科院分区:
医学1区
文献类型:
--
作者:
Hall MA;Xi J;Lor C;Dai S;Pearce R;Dailey WP;Eckenhoff RG

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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, GABAA 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.
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影响因子: 3.6
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