Characterization of rat transient receptor potential vanilloid 1 receptors lacking the N-glycosylation site N604.
Whole-cell patch-clamp recordings were performed on HEK293 cells transiently transfected with the rat (r) wild-type transient receptor potential vanilloid 1 (TRPV1) (rTRPV1) receptor or with a mutant that lacks the potential N-glycosylation site at position N604 (rTRPV1-N604T). Replacement of Asn by Thr (N604T) depressed the maximum of the concentration-response curve for capsaicin and decreased the EC50 value of this agonist. Further, such a manipulation modified the sensitivity to the TRPV1 receptor-antagonist capsazepine and altered the dependence of the capsaicin effect on extracellular pH. Hence, glycosylation may affect the basic functional characteristics of the rTRPV1 receptor channel in accordance with the knowledge that N-glycosylation may regulate ligand binding or gating properties of ionotropic neurotransmitter receptors.
Wirkner
Kerstin
K
Rudolf-Boehm Institute of Pharmacology and Toxicology, University of Leipzig, Haertelstrasse 16-18, D-04107 Leipzig, Germany. wirk@medizin.uni-leipzig.de
Hognestad
Huge
H
Jahnel
Ricarda
R
Hucho
Ferdinand
F
Illes
Peter
P
D000704:Analysis of Variance; D000818:Animals; D001216:Asparagine / Q000235:genetics*; D002211:Capsaicin / Q000031:analogs & derivatives / Q000494:pharmacology; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D004307:Dose-Response Relationship, Radiation; D004347:Drug Interactions; D004558:Electric Stimulation / Q000379:methods; D006031:Glycosylation; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007473:Ion Channels / Q000235:genetics / Q000378:metabolism* / Q000502:physiology; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology / Q000528:radiation effects; D018408:Patch-Clamp Techniques / Q000379:methods; D017354:Point Mutation; D051381:Rats; D050916:TRPV Cation Channels; D013912:Threonine / Q000235:genetics*; D014162:Transfection / Q000379:methods
D007473:Ion Channels; D050916:TRPV Cation Channels; C493922:Trpv1 protein, rat; D013912:Threonine; D001216:Asparagine; C071423:capsazepine; D002211:Capsaicin