Vortioxetine

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

Vortioxetine (Lu AA21004) 是一种多模式血清素能化合物，抑制 5-HT1A、5-HT1B、5-HT3A、5-HT7 受体和 SERT，IC50 分别为 15 nM、33 nM、3.7 nM、19 nM 和 1.6 nM。

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.(In Vitro):Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT. Vortioxetine is a partial h5-HT1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Vortioxetine binds to the r5-HT7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay.(In Vivo):Vortioxetine (Lu AA21004) occupies the r5-HT1B receptor and rSERT (ED50= 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT3 receptor antagonist. Vortioxetine significantly increases cell proliferation and cell survival and stimulates maturation of immature granule cells in the sub granular zone of the dentate gyrus of the hippocampus after 21 days of treatment. Vortioxetine does not cause cognitive or psychomotor impairment.

Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT. Vortioxetine is a partial h5-HT 1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Vortioxetine binds to the r5-HT 7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay.

Vortioxetine (Lu AA21004) occupies the r5-HT1B receptor and rSERT (ED50= 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT3 receptor antagonist. Vortioxetine significantly increases cell proliferation and cell survival and stimulates maturation of immature granule cells in the sub granular zone of the dentate gyrus of the hippocampus after 21 days of treatment. Vortioxetine does not cause cognitive or psychomotor impairment.

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Endocrinology/Hormones

5-HT Receptor

5-HT1A| 5-HT1B| 5-HT3A| 5-HT7| SERT

Neurological Disease

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508233-74-7

298.45

C18H22N2S

>98% (HPLC)

DMSO, Ethanol: 200 mM

CC1=CC(C)=C(SC2=CC=CC=C2N2CCNCC2)C=C1

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(-20℃)

With Ice Pack

≥ 2 years