Source:http://linkedlifedata.com/resource/pubmed/id/11937340
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
2002-4-8
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pubmed:abstractText |
A series of secondary face modified cyclodextrins (CDs) were synthesised with the aim of constructing host molecules capable of forming host-guest complexes with neuromuscular blockers, especially with rocuronium bromide. Perfacial 2-O-substitution of gamma-CD with 4-carboxybenzyl resulted in a CD host molecule 1 that forms a 1:1 binary complex with rocuronium bromide (K(a) 6.2 x 10(5) M(-1)). The biological activities of this compound and other derivatives as reversal agents of rocuronium bromide were examined in vitro (mouse hemi-diaphragm) and in vivo (anaesthetized guinea pigs). The host molecule 1 was found to exert potent reversal activity (ED(50) 0.21 micromol/kg, iv) against rocuronium-induced neuromuscular block, and thus proved the viability of using host molecules as antidotes of a biologically active compound.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1819-27
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11937340-Androstanols,
pubmed-meshheading:11937340-Animals,
pubmed-meshheading:11937340-Cyclodextrins,
pubmed-meshheading:11937340-Diaphragm,
pubmed-meshheading:11937340-Guinea Pigs,
pubmed-meshheading:11937340-Male,
pubmed-meshheading:11937340-Mice,
pubmed-meshheading:11937340-Molecular Structure,
pubmed-meshheading:11937340-Muscle Relaxation,
pubmed-meshheading:11937340-Neuromuscular Blockade,
pubmed-meshheading:11937340-Neuromuscular Nondepolarizing Agents,
pubmed-meshheading:11937340-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide.
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pubmed:affiliation |
Department of Medicinal Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, Scotland, UK.
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pubmed:publicationType |
Journal Article,
In Vitro
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