NNC 05-2090 hydrochloride

Research use only, not for human use.

NNC 05-2090 is a potent selective GABA transporter inhibitor of mGAT2 with Ki of 1.4 uM.

NNC 05-2090 is a potent selective GABA transporter inhibitor of mGAT2 with Ki of 1.4 uM; displays >10 fold selectivity over mGAT1, mGAT3 and mGAT4, also has alpha 1- and D2-receptor affinity of 266 and 1632 nM, respectively; inhibits 3HGABA uptake into synaptosomes from cerebral cortex with IC50 of 4.4 uM; significantly reduces generalized seizure severity and afterdischarge duration in rats.

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Animal Model:Partial sciatic nerve ligation (PSL) mice with mechanical allodynia Dosage:0.01, 0.1 and 0.3 mg/kg Administration:Intraperitoneal injection or intrathecal injection; 0.1 mg/kg, once Result:Dose-dependently reversed mechanical allodynia in PSL model mice by both intraperitoneal injection and intrathecal injection.

NNC05-2090

Membrane Transporter/Ion Channel

GAT

GAT

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184845-18-9

451.01

C27H31ClN2O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (221.73 mM)

COC1=CC=CC=C1C2(CCN(CC2)CCCN3C4=CC=CC=C4C5=CC=CC=C53)O.Cl

1-[3-(9H-Carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-4-piperidinol hydrochloride

(-20℃)

With Ice Pack

≥ 2 years