Selective Relaxant Binding Agent
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Selective relaxant binding agents (SRBAs) are a new class of
drug A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
s that selectively encapsulates and binds neuromuscular blocking agents (NMBAs). The first drug introduction of an SRBA is sugammadex. Sugammadex is a modified gamma cyclodextrin that specifically encapsulates and binds the aminosteroid NMBAs: rocuronium> vecuronium>> pancuronium. SRBAs exert a chelating action that effectively terminates an NMBA ability to bind to
nicotinic receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ner ...
s.


Discovery of SRBAs

The discovery of SRBA as a new class of drug is the result of work done by Organon laboratories at the
Newhouse research site The Newhouse Research Site is a drug research facility situated east of Glasgow in central Scotland. It is located beside the M8 motorway in Newhouse, North Lanarkshire. The site is an early drug discovery research centre with a track record o ...
in Scotland. Cyclodextrins were explored as a means to solubilize rocuronium bromide (a steroidal NMBA) in a neutral aqueous solution. Upon creating numerous modified cyclodextrins, one particular molecule was found to possess extremely high affinity for the rocuronium molecule. Originally known as Org25969, it is now generically named sugammadex sodium.


References

{{Acetylcholine receptor modulators Anesthesia Antidotes Polysaccharides