4-Iodopropofol Explained

4-Iodopropofol is a drug derived from the commonly used sedative anaesthetic agent, propofol. 4-Iodopropofol has similar effects to propofol on isolated receptors, acting primarily as a GABAA positive modulator and sodium channel blocker,[1] [2] [3] [4] but when given to animals it has only anxiolytic and anticonvulsant effects, lacking the strong sedative-hypnotic profile of propofol.[5]

Notes and References

  1. Trapani G, Latrofa A, Franco M, Altomare C, Sanna E, Usala M, Biggio G, Liso G . 6 . Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors . Journal of Medicinal Chemistry . 41 . 11 . 1846–54 . May 1998 . 9599235 . 10.1021/jm970681h .
  2. Lingamaneni R, Krasowski MD, Jenkins A, Truong T, Giunta AL, Blackbeer J, MacIver MB, Harrison NL, Hemmings HC . 19229035 . 6 . Anesthetic properties of 4-iodopropofol: implications for mechanisms of anesthesia . Anesthesiology . 94 . 6 . 1050–7 . June 2001 . 11465597 . 10.1097/00000542-200106000-00020 . free .
  3. Krasowski MD, Hong X, Hopfinger AJ, Harrison NL . 4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor . Journal of Medicinal Chemistry . 45 . 15 . 3210–21 . July 2002 . 12109905 . 2864546 . 10.1021/jm010461a .
  4. Haeseler G, Karst M, Foadi N, Gudehus S, Roeder A, Hecker H, Dengler R, Leuwer M . 6 . High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues . British Journal of Pharmacology . 155 . 2 . 265–75 . September 2008 . 18574460 . 2538694 . 10.1038/bjp.2008.255 .
  5. Sanna E, Motzo C, Usala M, Serra M, Dazzi L, Maciocco E, Trapani G, Latrofa A, Liso G, Biggio G . 6 . Characterization of the electrophysiological and pharmacological effects of 4-iodo-2,6-diisopropylphenol, a propofol analogue devoid of sedative-anaesthetic properties . British Journal of Pharmacology . 126 . 6 . 1444–54 . March 1999 . 10217539 . 1565920 . 10.1038/sj.bjp.0702449 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "4-Iodopropofol".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.