Screening for therapeutic activity or selectivity profiling off-target liability
Neurotransmitter transporters, especially biogenic amine transporters, have been a highly successful target class for clinical therapeutics. First generation Selective Serotonin Re-Uptake inhibitors (SSRIs) are one of the most recognized class of drugs to treat depression. While next generation anti-depressants with polypharmacology (activity across multiple targets) for serotonin and norepinephrine may offer better clinical activity.
Like most drug targets, unwanted interaction with neurotransmitter transporters may lead to adverse reactions. Therefore, profiling compound activity against neurotransmitter transporters is also important for general liability assessment.
Eurofins, through the expertise of Cerep and Panlabs, have both binding and cellular uptake assays to test compounds for interaction against this class of clinically important targets.
Advantages of neurotransmitter transporter screening with Eurofins:
Figures 1 and 2. Orthogonal assays to identify compounds that interact with serotonin transporter
Reference compounds were tested in concentration curves for their ability to inhibit 5-HT uptake by serotonoin transporter in brain synaptosomes (left panel) as well bind to human recombinant 5-HT transporter (right panel).