Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-44121
J Med Chem 2011 Dec 08;5423:8124-35. doi: 10.1021/jm200943f.
Show Gene links Show Anatomy links

p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol.

Stewart DS , Savechenkov PY , Dostalova Z , Chiara DC , Ge R , Raines DE , Cohen JB , Forman SA , Bruzik KS , Miller KW .


???displayArticle.abstract???
We synthesized 2,6-diisopropyl-4-[3-(3-methyl-3H-diazirin-3-yl)propyl]phenol (p-(4-azipentyl)propofol), or p-4-AziC5-Pro, a novel photoactivable derivative of the general anesthetic propofol. p-4-AziC5-Pro has an anesthetic potency similar to that of propofol. Like propofol, the compound potentiates inhibitory GABA(A) receptor current responses and allosterically modulates binding to both agonist and benzodiazepine sites, assayed on heterologously expressed GABA(A) receptors. p-4-AziC5-Pro inhibits excitatory current responses of nACh receptors expressed in Xenopus oocytes and photoincorporates into native nACh receptor-enriched Torpedo membranes. Thus, p-4-AziC5-Pro is a functional general anesthetic that both modulates and photoincorporates into Cys-loop ligand-gated ion channels, making it an excellent candidate for use in identifying propofol binding sites.

???displayArticle.pubmedLink??? 22029276
???displayArticle.pmcLink??? PMC3580944
???displayArticle.link??? J Med Chem
???displayArticle.grants??? [+]


References [+] :
Alifimoff, Anaesthetic potencies of primary alkanols: implications for the molecular dimensions of the anaesthetic site. 1989, Pubmed