4-Iodopropofol
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| ECHA InfoCard | 100.220.512 |
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| Formula | C12H17IO |
| Molar mass | 304.167 g/mol g·mol−1 |
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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]
References
- ^ Trapani, G; Latrofa, A; Franco, M; Altomare, C; Sanna, E; Usala, M; Biggio, G; Liso, G (1998). "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. doi:10.1021/jm970681h. PMID 9599235.
- ^ Lingamaneni, R; Krasowski, MD; Jenkins, A; Truong, T; Giunta, AL; Blackbeer, J; MacIver, MB; Harrison, NL; Hemmings Jr, HC (2001). "Anesthetic properties of 4-iodopropofol: implications for mechanisms of anesthesia". Anesthesiology. 94 (6): 1050–7. doi:10.1097/00000542-200106000-00020. PMID 11465597.
- ^ Krasowski, MD; Hong, X; Hopfinger, AJ; Harrison, NL (2002). "4D-QSAR Analysis of a Set of Propofol Analogues: Mapping Binding Sites for an Anesthetic Phenol on the GABAA Receptor". Journal of Medicinal Chemistry. 45 (15): 3210–21. doi:10.1021/jm010461a. PMC 2864546. PMID 12109905.
- ^ Haeseler, G; Karst, M; Foadi, N; Gudehus, S; Roeder, A; Hecker, H; Dengler, R; Leuwer, M (2008). "High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues". British Journal of Pharmacology. 155 (2): 265–75. doi:10.1038/bjp.2008.255. PMC 2538694. PMID 18574460.
- ^ Sanna, E; Motzo, C; Usala, M; Serra, M; Dazzi, L; MacIocco, E; Trapani, G; Latrofa, A; Liso, G; Biggio, G (1999). "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. doi:10.1038/sj.bjp.0702449. PMC 1565920. PMID 10217539.