GAT
GABA is the major inhibitory neurotransmitter in the brain and GABA re-uptake transport is one of the several pathways in the complex regulation of GABA activity. The first GABA transporter was GAT-1. The rat GAT, human GAT and mouse GAT are highly homologous (= 97%) proteins consisting of 599 amino acids. The proteins are termed rGAT-1, hGAT-1 and mGAT-1 respectively. Two other GABA transporters from rat brain related to GAT-1 but with distinct homology and pharmacological properties have been cloned, expressed in mammalian cells and named GAT-2 and GAT-3 respectively. Transporters function as molecularshuttles, transferring substrates across the membrane one moleculeat a time,then going back for more. GABA transporters belong to the family of Na+- and Cl-- coupled transporters, so named because these ions are co-transported with substrate. GABA transporters play a fundamental role in regulating extrasynaptic GABA levels, with inhibition of astroglial transporters being a critical target with anticonvulsant potential.
References
1.Soudijn W, et al. Curr Med Chem. 2000;7(10):1063–1079.
2.Borden LA. Neurochem Int. 1996;29(4):335–356.
3.Schousboe A, et al. Neurochem Res. 2014;39(10):1980–1987.
References
1.Soudijn W, et al. Curr Med Chem. 2000;7(10):1063–1079.
2.Borden LA. Neurochem Int. 1996;29(4):335–356.
3.Schousboe A, et al. Neurochem Res. 2014;39(10):1980–1987.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(62)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(64)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Potassium Channel(0)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
GAT
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DCBS152A
产品货号 : M17022
cas no: ——
DCBS152A 是 GABAA 受体的一种有效的功能选择性负调节剂,位于某些受体亚型的调节 PQ 位点。 -
NS11394
产品货号 : M16805
cas no: 951650-22-9
一种有效的、亚型选择性的、口服的 GABAA 受体正调节剂。 -
AZD-7325
产品货号 : M16745
cas no: 942437-37-8
AZD-7325 是一种有效的 α2/3 功能选择性部分 GABAA 受体调节剂,pKi 为 9.51。 -
AZD6280
产品货号 : M16744
cas no: 942436-93-3
AZD6280 是一种有效的 α2/3 功能选择性部分 GABAA 受体调节剂,pKi 为 7.7。 -
4-Amino-3-hydroxybutyric Acid
产品货号 : M16625
cas no: 924-49-2
改善学习或记忆力的药物 [US6803366]γ 羟基丁酸,通常缩写为 GHB.