| Neurochemicals | Signal Transduction Agents | Peptides | Biochemicals | |
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High Performance Life Science Reagents |
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Neurotransmitter Uptake Inhibitors
Most neurotransmitters are removed from the synaptic cleft by neurotransmitter transporters in a process called reuptake (uptake). Without reuptake, neurotransmitters can continue to stimulate or inhibit the firing of the postsynaptic neurons.
Glutamate Transporters
Glutamate is the main excitatory neurotransmitter in the CNS and glutamate receptors are present in the plasma membrane of most neurons and glial cells. Glutamate transporters are essential for terminating synaptic excitation and for maintaining extracellular glutamate concentrations below neurotoxic levels. The main transporters located on the plasma membrane are known as excitatory amino acid transporters (EAATs) and uptake is driven by Na+ and K+ gradients. Five EAATs have been cloned and are designated EAAT1-5.
Potent EAAT2 inhibitor
2652 l WAY 213613 Displays > 44-fold selectivity over EAAT1 and EAAT3 (IC50 values are 85, 3787 and 5004 nM for EAAT2, EAAT3 and EAAT1 respectively). Exhibits no activity towards ionotropic and metabotropic glutamate receptors. Glutamate Uptake Related Products: Dihydrokainic acid SYM 2081 DL-TBOA
GABA Transporters
Following release into the synapse, GABA is transported into presynaptic terminals and glial cells via Na+/Cl--dependent transporters. Four distinct GABA transporters have been cloned; the high affinity GAT-1, GAT-2 and GAT-3 and the low affinity BGT-1.
GABA uptake inhibitor
2747 l NNC 05-2090 Displays moderate selectivity for BGT-1. Anticonvulsive; inhibits sound-induced tonic and clonic convulsions in DBA/2 mice. GABA Uptake Related Products: NNC 711 SKF 89976A CI 966
Serotonin Transporters
Serotonin transporters are the important site of action for many therapeutic agents. Drugs that reduce the binding of serotonin to their transporters have been used in the treatment of depression, anxiety and some personality disorders. Selective serotonin-reuptake inhibitors (SSRIs) increase the extracellular level of serotonin, increasing the level available to bind the postsynaptic receptor.
Selective facilitator of 5-HT uptake
1972 l Tianeptine Has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenaline or dopamine uptake. Antidepressant, analgesic and neuroprotective following systemic administration in vivo. Serotonin Uptake Related Products: Lofepramine Dexfenfluramine |
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