Agonist-stimulated internalisation of the ligand-gated ion channel P2X(1) in rat vas deferens

Using cell surface biotinylation and Western blotting, we investigated the extent to which native P2X(1) receptors in rat vas deferens are internalise d after exposure to agonist, Exposure to 100 muM alpha,beta -meATP 30 min p rior and during a 10 min biotinylation period resulted in a similar to 50% reduction in the amount of biotinylated P2X(1) receptor indicating that act ivation of the receptor by agonist induces receptor internalisation, Furthe rmore, biotinylation under saturating conditions suggests that once interna lised, a rapid recycling of P2X(1) receptor back to the cell surface occurs . The physiological implications of these mechanisms in terms of receptor f unction are discussed, (C) 2001 Federation of European Biochemical Societie s, Published by Elsevier Science B.V. All rights reserved.