LY266097 hydrochloride

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

LY266097 hydrochloride 是一种选择性的 5-HT2B 受体拮抗剂，对 5-HT2A、5-HT2B、5-HT2C 的 pKi 分别为 7.7、9.8 和 7.6。5-HT2B 受体阻断有助于抑郁症的研究。

LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.

LY266097 is a highly selective 5-HT2B receptor antagonist with a pKi of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity over human 5-HT2C and 5-HT2A sites.

LY266097 (0.6?mg/kg for 2-day administration) rescues Escitalopram-induced decrease in dopamine (DA) .The administration of LY266097 alone or its addition on the last 3 days of a 14-day Escitalopram regimen increases pyramidal neuron firing and burst activity.Animal Model:Male Sprague-Dawley rats weighing 250-350?g Dosage:0.6?mg/kg Administration:Administered i.p. alone or concomitantly with Escitalopram (2?mg/kg) for 2 days Result:Short-term administration (0.6?mg/kg/day for 2 days; i.p.) alone had no effect on these parameters, its co-administration counteracted the inhibitory effect of escitalopram on the firing activity of DA neurons, resulting in a recovery to control level.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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172895-39-5

407.33

C21H24Cl2N2O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 62.5 mg/mL (153.44 mM; 超声助溶 (<60°C)

Cl.COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC

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(-20℃)

With Ice Pack

≥ 2 years