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货期：电询
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1781880-44-1
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电询
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GABAA receptor agent 2 TFA
CAS No. : 1781880-44-1
MCE 国际站：GABAA receptor agent 2 TFA
产品活性：GABAA receptor agent 2 TFA 是一种有效的高亲和力 GABAA 受体拮抗剂，IC50 为 24 nM (表达人 α1β2γ2 GABAA 的 tsA201 细胞)，Ki 为 28 nM (大鼠 GABAA 受体)。GABAA receptor agent 2 TFA 对四种人类 GABA 转运蛋白 (hGAT-1，hBGT-1，hGAT-2 和 hGAT-3) 无效。
研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：GABA Receptor
In Vitro: With the protonated piperidine nitrogen consistently placed to interact with β2 E155, only a simultaneous interaction with α1 R66 provided enough space above and below the ligand heteroaromatic ring to be compatible with the high affinity (0.022 μM) of the disubstituted GABAA receptor agent 2 (compound 19).
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文献和实验Characterization of the Picrotoxin Site of GABAA Receptors
, and competition assays (IC50 , K i determination) are included. Curr. Protoc. Pharmacol . 63:1.18.1?1.18.18. © 2013 by John Wiley & Sons, Inc. Keywords: GABAA receptor; picrotoxin binding site; allosteric regulation; convulsants
Electrophysiological Methods for Investigating Inhibitory Synaptic Plasticity
because it forms pores in the neuronal membrane that are permeable to monovalent cations and small uncharged molecules, but not to Cl− . Preserving the neuronal Cl− gradient is essential for recording native inhibitory GABAA receptor (GABAA R) currents
, T., Min, W., Schreiber, R., Hopkins, S.C., Campbell, U., and Paterson, N. 2011. Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2‐73 in rats trained to discriminate chlordiazepoxide
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