Cellular uptake assays and cellular release assays use live cells to examine the effects of compounds on receptor or transporter systems. They can determine a compound’s potency and efficacy. They can also be used to measure a compound’s transport into cells or efflux from cells. Our cell-based studies are conducted on either primary or immortalized cells lines. Cell culture is undertaken by us.
Cellular uptake assays can be used to measure the transport or internalization of labeled compounds into cells or the potency of unlabeled test compounds in inhibiting this transport.Labeled substances can be neurotransmitters, metabolites, drugs or proteins.
Determination of IC50values for test compounds against cellular uptake of radiolabeled neurotransmitters.
Determination of IC50values for test compounds against uptake of tritium or14C-labeled metabolites or drugs.
Cellular uptake and internalization of125I-labeled proteins.
Cellularrelease assays can be used to quantify the efflux of labeled substances from cells. Efflux can be via membrane ion channels, membrane transport or from cell lysis.
86Rb+rubidium efflux assay for quantification of drug effects on stimulation or inhibition of ligand-gated ion channel activity (nicotinic).
Efflux of3H and125I-labeled drugs from cells via transport.
51Cr chromium release assay for quantification of cell-mediated cytotoxicity.
Example Data: Cellular Uptake Assay
Inhibition of [3H]dopamine uptake into rat brain synaptosomes by the dopamine transport inhibitors, GBR 12909 and cocaine (top), shown in comparison with inhibition of [3H]mazindol binding (bottom).
Example Data: Cellular Release Assay
Inhibition of calcium-stimulated [3H]acetylcholine release from rat brain hippocampal synaptosomes by the CB1 receptor cannabinoid agonist, WIN 55212-2. The WIN 55212 inhibition was antagonized by the CB1 receptor antagonist, SR141716A.