Cellular Uptake
& Release

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.  

Applications include: 

• Determination of IC₅₀ values for test compounds against cellular uptake of radiolabeled neurotransmitters. 
• Determination of IC₅₀ values for test compounds against uptake of tritium or ¹⁴C-labeled metabolites or drugs. 
• Cellular uptake and internalization of ¹²⁵I-labeled proteins. 

Cellular release 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.  

Applications include:

• ⁸⁶Rb⁺ rubidium efflux assay for quantification of drug effects on stimulation or inhibition of  ligand-gated ion channel activity (nicotinic). 
• Efflux of ³H and ¹²⁵I-labeled drugs from cells via transport.