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盐酸阿洛司琼 /Alosetron HCl 98%

货号:A406003 同义名: GR 68755 Hydrochloride;GR 68755X Hydrochloride Ambeed 开学季,买赠积分,赢豪礼

Alosetron HCl is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.

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Alosetron HCl 化学结构 CAS号:122852-69-1
Alosetron HCl 化学结构
CAS号:122852-69-1
Alosetron HCl 3D分子结构
CAS号:122852-69-1
Alosetron HCl 化学结构 CAS号:122852-69-1
Alosetron HCl 3D分子结构 CAS号:122852-69-1
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Alosetron HCl 纯度/质量文件 产品仅供科研

货号:A406003 标准纯度: 98%
批次查询: 批次纯度:

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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

99%+
Venlafaxine 99%+
Fluvoxamine maleate 99%
Iloperidone 99%+
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 99%+
Trazodone 98+%
Clomipramine HCl 99%+
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

99%+
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

99%+
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

99%+
Latrepirdine 2HCl GluR 99%+
Fluoxetine hydrochloride 98%
Paroxetine hydrochloride AChR 99%+
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%+
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

99%
Agomelatine 99%+
Clozapine 99%+
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

99%+
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 99%+
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

99%+
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

99%+
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Alosetron HCl 生物活性

靶点
  • 5-HT3

描述 Alosetron HCl is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). It blocked the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons in vitro, with half-maximal inhibition at approximately 55 nmol/L. Alosetron attenuated the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs[1]. The protective effects of alosetron on TNBS (trinitrobenzenesulfonic acid)-induced colitis can be mediated by 5-HT3R (Hydroxytryptamine 3 receptor) [2]. Stress-induced visceral hyperalgesia was abolished when alosetron was injected intrathecally in intact rats or subcutaneously (0.3 mg/kg) in capsaicin-pretreated animals[3]. Alosetron (10-100 mg/kg) showed dose-dependent inhibition of CRF (corticotropin releasing factor)-induced defecation in rats[4]. The 5-HT(3)-receptor antagonist alosetron (30 mg/kg) and the histamine H(1)-receptor antagonist pyrilamine (5 mg/kg) markedly attenuated the response to luminal antigen[5].

Alosetron HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00067561 Irritable Colon ... 展开 >> Irritable Bowel Syndrome (IBS) 收起 << Phase 3 Completed - -
NCT01257477 - Completed - -
NCT00370032 Irritable Colon Phase 4 Completed - United Kingdom ... 展开 >> GSK Investigational Site London, United Kingdom, W1G 8HU 收起 <<

Alosetron HCl 参考文献

[1]Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000 Mar;59(3):511-8; discussion 519-20

[2]Motavallian A, Minaiyan M, Rabbani M, Mahzouni P, Andalib S. Anti-inflammatory effects of alosetron mediated through 5-HT3 receptors on experimental colitis. Res Pharm Sci. 2019 Jun;14(3):228-236

[3]Bradesi S, Lao L, McLean PG, Winchester WJ, Lee K, Hicks GA, Mayer EA. Dual role of 5-HT3 receptors in a rat model of delayed stress-induced visceral hyperalgesia. Pain. 2007 Jul;130(1-2):56-65

[4]Hirata T, Keto Y, Nakata M, Takeuchi A, Funatsu T, Akuzawa S, Sasamata M, Miyata K. Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats. Eur J Pharmacol. 2008 Jun 10;587(1-3):281-4

[5]Jiang W, Kreis ME, Eastwood C, Kirkup AJ, Humphrey PP, Grundy D. 5-HT(3) and histamine H(1) receptors mediate afferent nerve sensitivity to intestinal anaphylaxis in rats. Gastroenterology. 2000 Nov;119(5):1267-75

[6]Hirata T, Keto Y, Nakata M, Takeuchi A, Funatsu T, Akuzawa S, Sasamata M, Miyata K. Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats. Eur J Pharmacol. 2008 Jun 10;587(1-3):281-4

[7]Jiang W, Kreis ME, Eastwood C, Kirkup AJ, Humphrey PP, Grundy D. 5-HT(3) and histamine H(1) receptors mediate afferent nerve sensitivity to intestinal anaphylaxis in rats. Gastroenterology. 2000 Nov;119(5):1267-75

Alosetron HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.11mL

3.02mL

1.51mL

30.23mL

6.05mL

3.02mL

Alosetron HCl 技术信息

CAS号122852-69-1
分子式C17H19ClN4O
分子量 330.812
别名 GR 68755 Hydrochloride;GR 68755X Hydrochloride;Alosetron (hydrochloride);Lotronex;GR 68755X;GR 68755;GR 68755C;Alosetron Hydrochloride
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

H2O: 30 mg/mL(90.69 mM),配合低频超声助溶

动物实验配方
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