MolPharm xPharm- The Comprehensive Pharmacology Reference

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Fesik, S. W.
Right arrow Articles by Makriyannis, A.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Fesik, S. W.
Right arrow Articles by Makriyannis, A.

Geometric requirements for membrane perturbation and anesthetic activity. Conformational analysis of alphaxalone and delta 16- alphaxalone and 2H NMR studies on their interactions with model membranes

SW Fesik and A Makriyannis

2H NMR spectra were obtained for dimyristoylphosphatidylcholine multilamellar dispersions, perdeuterated in the fatty acid chains, in the presence and absence of two steroid analogs. The presence of the active anesthetic steroid alphaxalone results in consistently smaller 2H quadrupolar splittings (delta nu Q) for individual C2H2 segments of the fatty acid chains, indicating increased molecular disorder. In contrast, the inactive analog delta 16-alphaxalone causes no significant change in the 2H spectra of the phospholipid. The conformational analysis of alphaxalone and delta 16-alphaxalone in solution was carried out with the help of 1H and 13C high resolution NMR spectroscopy and the results were used to propose a molecular model for the interaction of the two steroids with membrane phospholipids. The model correlates the observed differences in the manner in which the two steroids interact with model membranes with differences in their respective conformations and provides a molecular basis for anesthetic steroid activity.

Volume 27, Issue 6, pp. 624-629, 06/01/1985
Copyright © 1985 by American Society for Pharmacology and Experimental Therapeutics




This article has been cited by other articles:


Home page
 ScienceHome page
S Schwarz, P Pohl, and G. Zhou
Steroid binding at sigma-"opioid" receptors
Science, December 22, 1989; 246(4937): 1635 - 1637.
[PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1985 by the American Society for Pharmacology and Experimental Therapeutics