ArticleBiophysical journal1988
Structure and location of amiodarone in a membrane bilayer as determined by molecular mechanics and quantitative x-ray diffraction.
Article in Biophysical journal, 1988. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 45 citations in OpenAlex.
- Structural determinants of drug partitioning in surrogates of phosphatidylcholine bilayer strata.Molecular pharmaceutics · 2013Article
- Does transbilayer diffusion have a role in membrane transport of drugs?Drug discovery today · 2012Review
- Modeling kinetics of subcellular disposition of chemicals.Chemical reviews · 2009Review
- Membrane hyperpolarization drives cation influx and fungicidal activity of amiodarone.The Journal of biological chemistry · 2009Article
- Comparing the lipid membrane affinity and permeation of drug-like acids: the intriguing effects of cholesterol and charged lipids.Pharmaceutical research · 2007Article
- Tetracaine-membrane interactions: effects of lipid composition and phase on drug partitioning, location, and ionization.Biophysical journal · 2007Article
- Interaction of the antiarrhythmic agents SR 33589 and amiodarone with the beta-adrenoceptor and adenylate cyclase in rat heart.British journal of pharmacology · 1995Article
- Interaction of the NMDA receptor noncompetitive antagonist MK-801 with model and native membranes.Biophysical journal · 1994Article
- Molecular basis for the inhibition of 1,4-dihydropyridine calcium channel drugs binding to their receptors by a nonspecific site interaction mechanism.Biophysical journal · 1992Article
- Models for the binding of amiodarone to the thyroid hormone receptor.Journal of computer-aided molecular design · 1992Article
- Rat cerebral cortical synaptoneurosomal membranes. Structure and interactions with imidazobenzodiazepine and 1,4-dihydropyridine calcium channel drugs.Biophysical journal · 1990Article
- Partitioning and location of Bay K 8644, 1,4-dihydropyridine calcium channel agonist, in model and biological membranes.Biophysical journal · 1989Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Amiodarone is a drug used in the treatment of cardiac arrhythmias and is believed to have a persistent interaction with cellular membranes. This study sought to examine the structure and location of amiodarone in a membrane bilayer. Amiodarone has a high membrane partition coefficient on the order of 10(6). Small angle x-ray diffraction was used to determine the position of the iodine atoms of amiodarone in dipalmitoylphosphatidylcholine (DPPC) lipid bilayers under conditions of low temperature and hydration where the DPPC bilayer is in the gel state. The time-averaged position of the iodine atoms was determined to be approximately 6 A from the center (terminal methyl region) of the lipid bilayer. A dielectric constant of kappa = 2, which approximates that of the bilayer hydrocarbon core region, was used in calculating a minimum energy structure for membrane-bound amiodarone. This calculated structure when compared with the crystal structure of amiodarone demonstrated that amiodarone could assume a conformation in the bilayer significantly different from that in the crystal. The results reported here are an attempt to correlate the position of a membrane-active drug in a lipid bilayer with its time-averaged conformation. This type of analysis promises to be of great use in the design of drugs with greater potency and higher specificity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.