TPA023

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TPA023 是一种有效的、α2/α3 亚型选择性、口服 GABAA 受体激动剂，对含有 α1、α2、α3 和 α5 的人类受体的 Kd 分别为 0.92、1.05 和 0.58 nM。

TPA023 is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors; shows much lower (50- to 2000-fold) affinities for α4 and α6 subtypes (Ki= 60 and 418 nM, respectively); demonstrates anxiolytic-like efficacy and anticonvulsant activity in mouse pentylenetetrazole seizure model.Anxiety Discontinued.

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TPA023 displays good receptor occupancy, when administered orally to rats. The dose of TPA023 resulting in 50% occupancy of rat brain GABAA receptors is 0.42 mg/kg, with the corresponding plasma concentration being 25 ng/mL. TPA023 is also efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection at a dose of 10 mg/kg i.p. (84% occupancy), with the ED50 of 0.19-0.41 nM, for protection against tonic convulsions (1.4 mg/kg i.p.) corresponding to around 50% occupancy. TPA023 (3 mg/kg p.o. in 0.5% methyl cellulose) shows anxiolytic-like effect on rats. TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys.

MK-0777

Membrane Transporter/Ion Channel

GAT

GAT

Neurological Disease

Anxiety

252977-51-8

395.442

C20H22FN7O

>98% (HPLC)

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FC1=CC=CC=C1C2=NN=C3C=C(C(C)(C)C)C(OCC4=NC=NN4CC)=NN32

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine

(-20℃)

With Ice Pack

≥ 2 years