CO-AGONISM IN DRUG-RECEPTOR INTERACTION - ILLUSTRATED BY THE NMDA RECEPTORS

The co-agonism between glutamate and glycine at the NMDA receptor rais es uncertainty about the estimation of the values of dissociation cons tants for agonists and antagonists and of efficacy for agonists. In th is article, Mauro Corsi, Paolo Fina and David Trist discuss how to ana lyse the interaction of the two agonists with the NMDA receptor by app lying an operational receptor model. Data simulation indicates that co -agonism can affect the potency as well as the efficacy of agonists. M oreover, the interaction of antagonists with the NMDA receptor can als o be affected, leading to altered estimation of the antagonist dissoci ation constants.