448961-39-5Relevant academic research and scientific papers
2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide.
Tarver, Gary J,Grove, Simon J A,Buchanan, Kirsteen,Bom, Anton,Cooke, Andrew,Rutherford, Samantha J,Zhang, Ming Qiang
, p. 1819 - 1827 (2002)
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.
