2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide.
Bioorg Med Chem
; 10(6): 1819-27, 2002 Jun.
Article
em En
| MEDLINE
| ID: mdl-11937340
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 11 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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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fármacos Neuromusculares não Despolarizantes
/
Ciclodextrinas
/
Androstanóis
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2002
Tipo de documento:
Article
País de afiliação:
Reino Unido