Transporter Assay

Transporters are transmembrane proteins that act as natural gatekeepers in and out of cells by facilitating the movement of substances, including drugs, across cell and organ membranes. Transporters can mediate drug disposition and can be major determinants of a drug’s pharmacokinetic, safety, and efficacy profile.

 

Monoamine neurotransmitters (MATs,) are central neurotransmitters. Including catecholamines and indoleamines. It functions as an integral plasma membrane transporter to regulate extracellular concentrations of monoamine neurotransmitters. Catecholamines include dopamine, norepinephrine, and epinephrine. Indoleamine is primarily serotonin. Due to their important role in neuronal signaling, MATs are often associated with drugs used to treat mental disorders, as well as recreational drugs.

 

Neurotransmitter Transporter Uptake Assay

Neurotransmitter transporters are one of the key components of synapses, they are present in the cell membranes of nerve endings, and their role is to terminate their action by retaking the released transmitters. Neurotransmitter transporters have emerged as an important class of drug targets because they play a key role in depression and neurodegenerative diseases (NDDs) such as Alzheimer’s disease and Parkinson’s disease.

 

LeadQuest Biotech use cell-based neurotransmitter transporter assay models that can assess the impact of drug candidates on transporter activity. Aimed to help with accelerate the hit-to-lead selection process by providing fast and efficient compound analysis services to determine the respective agonistic and inhibitory activities and the selectivity of the lead compounds for various drug targets.

 

Using a fluorescent substrate that mimics biogenic amine neurotransmitters, it enters cells through these specific transporters, resulting in an increase in intracellular fluorescence intensity.