Cucurbit[n]uril type hosts for the reversal of steroidal neuromuscular blocking agents.

Future Med Chem

Department of Chemistry, Queen's University, Kingston, Ontario, K7L 3N6, Canada.

Published: November 2013

The ideal neuromuscular blocking agent (NMBA) is regarded as being a non-depolarizing equivalent of succinylcholine, having a rapid onset and short duration of action, with minimal side effects. In the absence of a single drug, the administration of an aminosteroid NMBA, such as rocuronium, followed by reversal using an acetylcholinesterase inhibitor, such as neostigmine, is commonly employed. A different and safer approach to rapidly reversing the action of the NMBA, by encapsulating it with a macrocyclic or acyclic host molecule, such as the cyclodextrin sugammadex or more recently, cucurbituril-type hosts such as cyclic cucurbit[7]uril and the acyclic glycoluril tetramer calabadion 1, is described.

Download full-text PDF

Source
http://dx.doi.org/10.4155/fmc.13.164DOI Listing

Publication Analysis

Top Keywords

neuromuscular blocking
8
cucurbit[n]uril type
4
type hosts
4
hosts reversal
4
reversal steroidal
4
steroidal neuromuscular
4
blocking agents
4
agents ideal
4
ideal neuromuscular
4
blocking agent
4

Similar Publications

The combination of ultralong-acting neuromuscular block and subsequent on-demand rapid reversal may provide prolonged surgeries with improved conditions by omitting continuous or repetitive blocker administration, enabling a more stable and predictable hemodynamic profile and eliminating residual block. For this target, we prepared 19 imidazolium-incorporated tetracationic macrocycles. In vivo studies with rats revealed that one macrocycle (IMC-14) displays extremely high blocking activity.

View Article and Find Full Text PDF

Background: Aromatic L-amino acid decarboxylase (AADC) deficiency is a rare life-threatening inborn error of neurotransmitter biosynthesis. It is characterized by deficient biosynthesis of neurotransmitters dopamine and serotonin, leading to catecholamines deficiency and sympathetic deprivation, while the parasympathetic system remains functional. Since 2012, gene therapy has led to clinical improvements in symptoms and motor function with a severe phenotype.

View Article and Find Full Text PDF

Charcot first described ALS in 1869, but the specific mechanisms that mediate the disease pathology are still not clear. Intense research efforts have provided insight into unique neuroanatomical regions, specific neuronal populations and genetic associations for ALS and other neurodegenerative diseases; however, the experimental results also suggest a convergence of these events to common toxic pathways. We propose that common toxic pathways can be therapeutically targeted, and this intervention will be effective in slowing progression and improving patient quality of life.

View Article and Find Full Text PDF

Probing the properties of PTEN specific botulinum toxin type E mutants.

J Neural Transm (Vienna)

January 2025

Institut für Zellbiochemie, OE 4310, Medizinische Hochschule Hannover, 30623, Hannover, Germany.

Botulinum neurotoxins (BoNT) are established biopharmaceuticals for neuromuscular and secretory conditions based on their ability to block neurotransmitter release from neurons by proteolyzing specific soluble N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE) proteins. Recently, a mutant catalytic domain of serotype E (LC/E) exhibiting 16 mutations was reported to cleave the phosphatase and tensin homolog (PTEN). This molecule represents an attractive new target in neurons as several reports support PTEN knockdown as a strategy to stimulate axonal regeneration after injury.

View Article and Find Full Text PDF

Objective: To investigate the pharmacodynamics and pharmacokinetics of rocuronium administered by bolus injection to sevoflurane-anesthetized horses.

Study Design: Prospective, experimental, crossover study.

Animals: Five healthy adult Thoroughbred horses (body mass 368-470 kg, three females and two males).

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!