Photoactive analogues of the haloether anesthetics provide high-resolution features from low-affinity interactions
ACS chemical biology, 2006•ACS Publications
The difficulty in obtaining binding target and site information for low-affinity drugs, like the
inhaled anesthetics, has limited identification of their molecular effectors. Because such
information can be provided by photoactive analogues, we designed, synthesized, and
characterized a novel diazirnyl haloether that closely mimics isoflurane, the most widely
used clinical general anesthetic. This compound, H-diaziflurane, is a nontoxic, potent
anesthetic that potentiates GABA-gated ion channels in primary cultures of hippocampal …
inhaled anesthetics, has limited identification of their molecular effectors. Because such
information can be provided by photoactive analogues, we designed, synthesized, and
characterized a novel diazirnyl haloether that closely mimics isoflurane, the most widely
used clinical general anesthetic. This compound, H-diaziflurane, is a nontoxic, potent
anesthetic that potentiates GABA-gated ion channels in primary cultures of hippocampal …
The difficulty in obtaining binding target and site information for low-affinity drugs, like the inhaled anesthetics, has limited identification of their molecular effectors. Because such information can be provided by photoactive analogues, we designed, synthesized, and characterized a novel diazirnyl haloether that closely mimics isoflurane, the most widely used clinical general anesthetic. This compound, H-diaziflurane, is a nontoxic, potent anesthetic that potentiates GABA-gated ion channels in primary cultures of hippocampal neurons. Calorimetric and structural characterizations show that H-diaziflurane binds a model anesthetic host protein with similar energetics as isoflurane and forms photoadducts with residues lining the isoflurane binding site. H-diaziflurane will be immediately useful for identifying targets and sites important for the molecular pharmacology of the inhaled haloether anesthetics.
![](/scholar/images/qa_favicons/pubs.acs.org.png)
以上显示的是最相近的搜索结果。 查看全部搜索结果