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Alosetron HCl

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Chemical Structure| 122852-69-1 同义名 : GR 68755 Hydrochloride;GR 68755X Hydrochloride;Alosetron (hydrochloride);Lotronex;GR 68755X;GR 68755;GR 68755C;Alosetron Hydrochloride
CAS号 : 122852-69-1
货号 : A406003
分子式 : C17H19ClN4O
纯度 : 98%
分子量 : 330.812
MDL号 : MFCD03453647
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：
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].
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 <<
实验方案
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
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