Uncompetitive antagonist

Uncompetitive antagonists differ from non-competitive antagonists in that they require receptor activation by an agonist before they can bind to a separate allosteric binding site. This type of antagonism produces a kinetic profile in which "the same amount of antagonist blocks higher concentrations of agonist better than lower concentrations of agonist".[1] Memantine, used in the treatment of Alzheimer's disease, is an uncompetitive antagonist of the NMDA receptor.[2]

References

  1. ↑ Lipton SA (2004). "Failures and successes of NMDA receptor antagonists: molecular basis for the use of open-channel blockers like memantine in the treatment of acute and chronic neurologic insults". NeuroRx : the journal of the American Society for Experimental NeuroTherapeutics 1 (1): 101–10. doi:10.1602/neurorx.1.1.101. PMC 534915. PMID 15717010.
  2. ↑ Parsons CG, Stöffler A, Danysz W; Stöffler; Danysz (2007). "Memantine: a NMDA receptor antagonist that improves memory by restoration of homeostasis in the glutamatergic system — too little activation is bad, too much is even worse". Neuropharmacology 53 (6): 699–723. doi:10.1016/j.neuropharm.2007.07.013. PMID 17904591.
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