Molecular and cellular basis of praziquantel action in the cardiovascular system.

ABSTRACT: The anthelmintic drug praziquantel (PZQ) causes contraction of parasitic schistosomes as well as constriction of blood vessels within the mesenteric vasculature of the host where the adult blood flukes reside. The contractile action of PZQ on the vasculature is mediated by the activation of host serotonergic 5-HT_2B receptors (5-HT_2BRs). However, the molecular basis for PZQ interaction with these targets and the location of these 5-HT_2B receptors in the vessel wall have not been experimentally defined. Evaluation of a PZQ docking pose within the 5-HT_2BR orthosteric site, using both Ca²⁺ reporter and bioluminescence resonance energy transfer (BRET) assays, identified residues F340^6.51 and F341^6.52 (transmembrane hel

SUBMITTER: Yahya NA 

PROVIDER: S-EPMC9942900 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature