NNC 711 - CAS 145645-62-1
Category: Inhibitor
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GABA Receptor
NNC 711 is a GABA uptake inhibitor by GAT-1 with IC50 values of 0.04, 171, 1700 and 622 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1. NNC 711 is an anticonvulsantagent.
≥99% by HPLC
NNC 711; NNC711; NNC-711; 1,2,5,6-Tetrahydro-1-[2-[[(diphenylmethylene)amino]oxy]ethyl]-3-pyridinecarboxylic acid hydrochloride
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1.Different mechanisms regulate IPSC kinetics in early postnatal and juvenile hippocampal granule cells.
Draguhn A;Heinemann U J Neurophysiol. 1996 Dec;76(6):3983-93.
1. Monosynaptic inhibitory postsynaptic currents (IPSCs) were recorded from early postnatal and juvenile dentate granule cells in rat brain slices at room temperature. The focally evoked currents were mediated by gamma-aminobutyric acid-A (GABAA) receptors. 2. IPSCs were characterized by a steep rising phase and a slower, monoexponential decay time course. The decay time constant was potential dependent and average values ranged from 33 ms at a holding potential of -60 mV to 58 ms at a holding potential of +40 mV. 3. IPSCs were studied in tissue from animals between postnatal day (p) 3 and p25. All kinetic parameters as well as the mean current amplitude were unchanged during this ontogenetic period. 4. In juvenile granule cells from animals aged 13-16 days, addition of the GABA uptake blocker (R)-N-[4,4-bis (3-methyl-2-thienyl) but-3-en1-yl] nipecotic acid (tiagabine) (10 microM) prolonged the decaying phase of the IPSCs. The current decay remained monoexponential but the time constant increased to 250% of control values. Mean current amplitudes remained largely unchanged. 5. In contrast, tiagabine had no effect on IPSCs in early postnatal tissuĕ. The decay time constant remained unchanged in cells recorded from animals aged p4-p6.
2.GABA transporters regulate tonic and synaptic GABA
Moldavan M;Cravetchi O;Allen CN J Neurophysiol. 2017 Dec 1;118(6):3092-3106. doi: 10.1152/jn.00194.2017. Epub 2017 Aug 30.
GABA is a principal neurotransmitter in the hypothalamic suprachiasmatic nucleus (SCN) that contributes to intercellular communication between individual circadian oscillators within the SCN network and the stability and precision of the circadian rhythms. GABA transporters (GAT) regulate the extracellular GABA concentration and modulate GABA;A; receptor (GABA;A;R)-mediated currents. GABA transport inhibitors were applied to study how GABA;A;R-mediated currents depend on the expression and function of GAT. Nipecotic acid inhibits GABA transport and induced an inward tonic current in concentration-dependent manner during whole cell patch-clamp recordings from SCN neurons. Application of either the selective GABA transporter 1 (GAT1) inhibitors NNC-711 or SKF-89976A, or the GABA transporter 3 (GAT3) inhibitor SNAP-5114, produced only small changes of the baseline current. Coapplication of GAT1 and GAT3 inhibitors induced a significant GABA;A;R-mediated tonic current that was blocked by gabazine. GAT inhibitors decreased the amplitude and decay time constant and increased the rise time of spontaneous GABA;A;R-mediated postsynaptic currents. However, inhibition of GAT did not alter the expression of either GAT1 or GAT3 in the hypothalamus.
3.Evaluation of GABA uptake in subcellular fractions of bovine frontal cortex and brainstem.
Höfner G;Wanner KT Neurosci Lett. 2004 Jun 24;364(1):53-7.
GABA uptake as well as the distribution of GAT-1, GAT-2 and GAT-3 were investigated in bovine brain membrane fractions. GABA uptake was characterised by kinetic constants and IC50-values for a series of known inhibitors in subcellular fractions of frontal cortex and brainstem obtained by subsequent centrifugations on sucrose gradients. Additionally, the immunoreactivity for rGAT-1, rGAT-2 and rGAT-3 antibodies was studied in these fractions. The pharmacological profile for GABA uptake inhibition as well as results from immunoblotting indicated that GABA uptake in a selected subcellular fraction of frontal cortex (P2B) is almost exclusively due to GAT-1 whereas GABA uptake performed with a selected subcellular fraction of brainstem (P2A) in the presence of NNC 711 is mainly attributable to GAT-3.
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CAS 145645-62-1 NNC 711

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