Journal article
Photoactive analogues of the haloether anesthetics provide high-resolution features from low-affinity interactions
ACS chemical biology, v 1(6), pp 377-384
21 Jul 2006
PMID: 17163775
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
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.
Metrics
Details
- Title
- Photoactive analogues of the haloether anesthetics provide high-resolution features from low-affinity interactions
- Creators
- Jin Xi - Department of Anesthesiology & Critical Care, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USARenyu LiuMatthew J RossiJay YangPatrick J LollWilliam P DaileyRoderic G Eckenhoff
- Publication Details
- ACS chemical biology, v 1(6), pp 377-384
- Publisher
- American Chemical Society; Washington, DC
- Grant note
- NS-45718 / NINDS NIH HHS GM-55876 / NIGMS NIH HHS Y1 GM-0080-03 / NIGMS NIH HHS
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Biochemistry and Molecular Biology
- Web of Science ID
- WOS:000243869600017
- Scopus ID
- 2-s2.0-39049192841
- Other Identifier
- 991014878123404721
UN Sustainable Development Goals (SDGs)
This publication has contributed to the advancement of the following goals:
InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Collaboration types
- Domestic collaboration
- Web of Science research areas
- Biochemistry & Molecular Biology