Alosetron HCl | GR 68755 Hydrochloride | 5-HT3 Receptor Antagonist

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Alosetron HCl/盐酸阿洛司琼 {[allProObj[0].p_purity_real_show]}

货号：A406003 同义名： GR 68755 Hydrochloride; GR 68755X Hydrochloride

Alosetron hydrochloride (GR 68755C) 是一种高效、高选择性的 5-HT₃ 受体拮抗剂（IC50 ≈ 55 nM），可阻断 5-HT₃ 介导的豚鼠肌间和粘膜下神经元快速去极化，减轻犬直肠扩张引起的内脏伤害性反应，并具有抗炎活性，常用于肠易激综合征（IBS）相关机制研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Alosetron HCl/盐酸阿洛司琼化学结构
CAS号：122852-69-1

Alosetron HCl/盐酸阿洛司琼 3D分子结构
CAS号：122852-69-1

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Alosetron HCl/盐酸阿洛司琼纯度/质量文件产品仅供科研

货号：A406003 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

5-羟色胺受体亚型比较

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 (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								98%
Venlafaxine	✔								99%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								97%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	99%
Fluoxetine HCl	✔								99.5%
Paroxetine HCl	✔							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						95%
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 (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						98%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	99%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron HCl dihydrate				✔					98%
VUF10166				++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM					99%+
Azasetron HCl				++++ 5-HT3, IC50: 0.33 nM					99%
Asenapine maleate		+++ 5-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 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		97%
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
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-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		95%
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/盐酸阿洛司琼生物活性

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/盐酸阿洛司琼临床研究

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/盐酸阿洛司琼参考文献

[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/盐酸阿洛司琼实验方案

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/盐酸阿洛司琼技术信息

CAS号	122852-69-1
分子式	C₁₇H₁₉ClN₄O
分子量	330.81
SMILES Code	O=C1N(CC2=C(C)N=CN2)CCC(N3C)=C1C4=C3C=CC=C4.[H]Cl
MDL No.	MFCD03453647

别名	GR 68755 Hydrochloride; GR 68755X Hydrochloride; Alosetron (hydrochloride); Lotronex; GR 68755X; GR 68755; GR 68755C; Alosetron Hydrochloride
运输	蓝冰
InChI Key	FNYQZOVOVDSGJH-UHFFFAOYSA-N
Pubchem ID	60758

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

细胞实验：

H₂O: 30 mg/mL(90.69 mM)，配合低频超声助溶

Alosetron HCl/盐酸阿洛司琼 {[allProObj[0].p_purity_real_show]}

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Alosetron HCl/盐酸阿洛司琼纯度/质量文件产品仅供科研

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