化学
异丙酚
麻醉剂
γ-氨基丁酸受体
兴奋剂
爪蟾
药理学
受体
配体(生物化学)
立体化学
生物化学
麻醉
生物
基因
医学
作者
Deirdre S. Stewart,Pavel Y. Savechenkov,Zuzana Dostálová,David C. Chiara,Rile Ge,Douglas E. Raines,Jonathan B. Cohen,Stuart A. Forman,Karol S. Bruzik,Keith W. Miller
摘要
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.
科研通智能强力驱动
Strongly Powered by AbleSci AI