Bis- and Mixed-Tetrahydroisoquinolinium Chlorofumarates:  New Ultra-Short-Acting Nondepolarizing Neuromuscular Blockers

Boros, Eric E.; Bigham, Eric C.; Boswell, G. Evan; Mook, Robert A.; Patel, Sanjay; Savarese, John J.; Ray, John A.; Thompson, James B.; Hashim, Mir A.; Wisowaty, James C.; Feldman, Paul L.; Sámano, Vicente

doi:10.1021/jm980597h

Cited by 33 publications

(17 citation statements)

References 15 publications

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“…Previously in experimental animals we could demonstrate that the onset and recovery characteristics of structurally similar bisquaternary tropinyl diesterstype agents, e.g. TAAC3 were also faster and shorter than reported in the literature for the new experimental neuromuscular relaxant GW280430A (Boros et al, 1999).…”

Section: Functional Aspectsmentioning

confidence: 66%

Quaternary derivatives of granatanol diesters: Potent, ultrashort acting non-depolarizing neuromuscular relaxants

et al. 2006

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Section: Functional Aspectsmentioning

confidence: 66%

Quaternary derivatives of granatanol diesters: Potent, ultrashort acting non-depolarizing neuromuscular relaxants

et al. 2006

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“…The present longer duration of action (7.1 min), a twice as long onset (96 s) as the latter, and a selectivity index similar to that of mivacurium (SI =20) [44]. Replacement of the trimethoxybenzyl groups in 15 by the equally substituted phenyl moieties to give 16 produced a ca.…”

Section: Tetrahydroisoquinolinium Analoguesmentioning

confidence: 86%

“…A number of trisubstituted benzyl derivatives was also examined. Notable compound is the 3,5-dimethoxy-4-acetoxy derivative (44) with the octylene spacer having the fastest onset (0.4 min) among the entire series. The effect of several structural changes of the tropane ring system was also explored.…”

Section: Bistropinyl Diester Analoguesmentioning

confidence: 99%

Recent Advances in Neuromuscular Blocking Agents

Zlotos

2005

MRMC

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Since the introduction of (+)-tubocurarine into anaesthetic and surgical practice (1942), a number of non-depolarizing neuromuscular blocking agents (NMBs) with improved pharmacological properties have been developed during the last sixty years. However, after withdrawal of rapacuronium from clinical use, there is still a need for an ultra-short acting non-depolarizing muscle relaxant with rapid onset as substitution for the polarizing suxamethonium, which has several undesirable side-effects. In this paper, structure-activity relationships within four different series of NMBs (tetrahydroisoquinolinium, bistropinyl diester, aminosteroid, and amino peptide analogues) published in this millennium have been reviewed. The NMB properties of the most promising drug candidates from each series were discussed and compared to those of the already existing muscle relaxants.

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“…Although seminal work related to gantacurium and related compounds was accomplished in the early 1990s, it was not until 1996 that gantacurium (initially GW280430) was identified and subsequently synthesized [9][10][11][12]. In contrast to the symmetric structure of many enantiomericbisquaternary compounds that have been studied, gantacurium is an asymmetric bis-onium ester of a-chlorofumaric acid (Fig.…”

Section: Introductionmentioning

confidence: 99%