Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay.
The human glycine receptor subtypes alpha1beta and alpha2 have been expressed stably in HEK293 cells, and the functional characteristics of the receptors have been characterised in the FLIPR Membrane Potential Assay. The pharmacological properties obtained for nine standard ligands at the two receptors in this assay were found to be in good agreement with those from electrophysiology studies of the receptors expressed in Xenopus oocytes or mammalian cell lines. Hence, this high throughput screening assay will be of great use in future pharmacological studies of glycine receptors, particular in the search for novel compound structures acting at them.
Jensen
Anders A
AA
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen, Denmark. aaj@dfuni.dk
D000731:Androstanes / Q000494:pharmacology; D001378:Azasteroids / Q000494:pharmacology; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D005453:Fluorescence; D005998:Glycine / Q000494:pharmacology; D018684:Glycine Agents / Q000494:pharmacology*; D006801:Humans; D008564:Membrane Potentials / Q000187:drug effects; D018408:Patch-Clamp Techniques; D010852:Picrotoxin / Q000494:pharmacology; D018009:Receptors, Glycine / Q000235:genetics / Q000502:physiology*; D013331:Strychnine / Q000031:analogs & derivatives / Q000494:pharmacology; D013654:Taurine / Q000494:pharmacology; D014162:Transfection; D015091:beta-Alanine / Q000494:pharmacology
D000731:Androstanes; D001378:Azasteroids; D005998:Glycine; D018684:Glycine Agents; D010852:Picrotoxin; D018009:Receptors, Glycine; D013331:Strychnine; D013654:Taurine; D015091:beta-Alanine; C083806:brucine; C032061:RU 5135