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2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide.

Abstract：

: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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tarver GJ,Grove SJ,Buchanan K,Bom A,Cooke A,Rutherford SJ,Zhang MQ

doi

10.1016/s0968-0896(02)00026-3

subject

Has Abstract

pub_date

2002-06-01 00:00:00

pages

1819-27

issue

6

eissn

0968-0896

issn

1464-3391

pii

S0968089602000263

journal_volume

10

pub_type

杂志文章

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