Prolonged inhibition of 5‐HT3 receptors by palonosetron results from surface receptor inhibition rather than inducing receptor internalization
British Journal of Pharmacology2013Vol. 169(6), pp. 1252–1262
Citations Over TimeTop 10% of 2013 papers
Abstract
Palonosetron acts as a pseudo-irreversible antagonist causing prolonged inhibition of 5-HT₃ receptors due to its very slow dissociation. In addition, an irreversible binding mode persists for at least 4 days. Allosteric receptor interactions appear to play a role in this phenomenon.
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