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GABA transporters are sodium- and chloride-dependent members of the solute carrier family 6 (SLC6) that mediate the rapid removal of GABA and maintain low extracellular levels. Four 12-TM domain transporters have been identified and localized to neurons and glia.
|Cat. No.||Product Name / Activity|
|1296||CI 966 hydrochloride|
|Selective inhibitor of GAT-1|
|Selective GAT-1 inhibitor|
|GABA uptake inhibitor; also inhibits glutamate release and blocks NaV channels|
|1081||SKF 89976A hydrochloride|
|Potent GAT-1 inhibitor; brain penetrant|
|GABA uptake inhibitor|
|GABA uptake inhibitor; also GABAA agonist and substrate for GABA-T|
|Selective GAT-1 inhibitor; anticonvulsant|
GABA transporters are sodium- and chloride-dependent members of the solute carrier family 6 (SLC6) that mediate the rapid removal of GABA and maintain low extracellular levels. Four 12-TM domain transporters (GAT-1, GAT-2, GAT-3 and BGT-1) have been identified and localized to neurons and glia.
While GAT-1, GAT-2, GAT-3 and BGT-1 bind GABA with varying affinities, they share structural motifs including 12-TM domains, extracellular glycosylation sites and intracellular consensus sites for phosphorylation. A vesicular transporter (VGAT) has also been identified. This member of the SCL32 family is both structurally and functionally distinct, containing 10-TM domains and being found in GABAergic and glycinergic neurons.
Some anticonvulsants have been reported to act upon the GABA transporters. There is evidence to suggest that GABA transporters are linked to epilepsy, affective disorders and schizophrenia.
Tocris offers the following scientific literature for GABA Transporters to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.
|Gene||Species||Gene Symbol||Gene Accession No.||Protein Accession No.|
|Tissue Localization1||Mainly neuronal cells in CNS||Epithelial, glial and neuronal cells (mainly CNS)||Mainly glial cells in CNS and retina||Probably mainly glial cells in CNS and kidney|
|Selected Inhibitors||IC50 (μM)|
|CI 966 (1296)||0.262||2972||3332||3002|
|(±)-Nipecotic acid (0236)||82||382||1062||23702|
|NNC 711 (1779)||0.042||1712||17002||6222|
|SKF 89976A (1081)||0.132||5502||9442||72102|
|(S)-SNAP 5114 (1561)||3883||213||53||1403|
IC50 values are for inhibition of [3H]-GABA uptake by cloned human GAT-1, rat GAT-2, human GAT-3 and human BGT-1.