SR 57227 hydrochloride是一种强效的serotonin type-3 (5-HT3)受体激动剂，能够穿过血脑屏障。
Cas No.:77145-61-0
Sample solution is provided at 25 µL, 10mM.
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SR 57227 hydrochloride is a potent serotonin type-3 (5-HT3) receptor agonist with the ability to cross the blood brain barrier [1]. SR 57227 hydrochloride can enhance the expression of c-Fos induced by fasting in the brainstem and hypothalamus of mice, and block the downregulation of proopiomelanocortin expression in the hypothalamus and tyrosine hydroxylase expression in the brain stem caused by fasting, thereby inhibiting the feeding behavior of mice[2]. SR 57227 hydrochloride is widely incorporated into the design of ionizable lipid to develop lipid nanoparticles (LNP) for systemic delivery of mRNA to the brain[3].
In vivo, SR 57227 hydrochloride treatment via intraperitoneal injection at a single dose (1mg/kg) for one hour can increase the locomotor activity of female mice and promote the vertical standing behaviors[4]. A single intraperitoneal injection of SR 57227 hydrochloride (10mg/kg) for 30 minutes reduced the pain-like behaviors in mice triggered by environmental cues[5]. Continuous intraperitoneal injection of SR 57227 hydrochloride (20mg/kg; twice a day) for 8 consecutive days significantly inhibited the death caused by spontaneous seizure in C57-DR mice[6]. A single intraperitoneal injection of SR 57227 hydrochloride (40mg/kg) at 30 minutes significantly reduced susceptibility to seizure-induced respiratory arrest (S-IRA) that leads to death in the DBA/1 mouse model of sudden unexpected death in epilepsy[7].
References:
[1] Bachy A, Héaulme M, Giudice A, et al. SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo[J]. European journal of pharmacology, 1993, 237(2-3): 299-309.
[2] Li B, Shao D, Luo Y, et al. Role of 5-HT3 receptor on food intake in fed and fasted mice[J]. PLoS One, 2015, 10(3): e0121473.
[3] Cao D, Hou X, Wang C, et al. Lipid nanoparticles for mRNA delivery in brain via systemic administration[J]. Science Advances, 2025, 11(33): eadw0730.
[4] Brookshire B R, Jones S R. Direct and indirect 5-HT receptor agonists produce gender-specific effects on locomotor and vertical activities in C57 BL/6J mice[J]. Pharmacology Biochemistry and Behavior, 2009, 94(1): 194-203.
[5] Nakamura Y, Sumi T, Mitani O, et al. SR 57227A, a serotonin type-3 receptor agonist, as a candidate analgesic agent targeting nociplastic pain[J]. Biochemical and biophysical research communications, 2022, 622: 143-148.
[6] Guo J, Min D, Farrell E K, et al. Enhancing the action of serotonin by three different mechanisms prevents spontaneous seizure‐induced mortality in Dravet mice[J]. Epilepsia, 2024, 65(6): 1791-1800.
[7] Faingold C L, Randall M, Zeng C, et al. Serotonergic agents act on 5-HT3 receptors in the brain to block seizure-induced respiratory arrest in the DBA/1 mouse model of SUDEP[J]. Epilepsy & Behavior, 2016, 64: 166-170.
SR 57227 hydrochloride是一种强效的serotonin type-3 (5-HT3)受体激动剂，能够穿过血脑屏障[1]。SR 57227 hydrochloride可增强禁食诱导的小鼠脑干和下丘脑中c-Fos的表达，并阻断禁食引起的下丘脑proopiomelanocortin表达下调和脑干tyrosine hydroxylase表达下调，从而抑制小鼠的进食行为[2]。SR 57227 hydrochloride被广泛用于可电离脂质的设计中，以开发用于将mRNA 全身递送至大脑的脂质纳米颗粒[3]。
在体内，单次腹腔注射SR 57227 hydrochloride（1mg/kg）一小时，可增加雌性小鼠的运动活性，并促进垂直站立行为[4]。单次腹腔注射SR 57227 hydrochloride（10mg/kg）30分钟，可减少由环境线索触发的小鼠疼痛样行为[5]。连续8天每天两次腹腔注射SR 57227 hydrochloride（20mg/kg），可显著抑制C57-DR小鼠因自发性癫痫发作导致的死亡[6]。在DBA/1小鼠癫痫猝死模型中，单次腹腔注射SR 57227 hydrochloride（40mg/kg）30分钟，可显著降低导致死亡的癫痫诱发呼吸暂停(S-IRA)的易感性[7]。
| Animal experiment [1]: | |
Animal models | Scn1a(+/−)/C57BL/6J (C57-DR) mice |
Preparation Method | C57-DR mice were kept in temperature-controlled (21°C-25°C) and humidity-maintained (40%-70%) rooms with a 12-h light/dark cycle. Water and food were provided freely. C57-DR mice were randomly assigned to the experimental or the vehicle control group. SR 57227 hydrochloride or vehicle (saline) was intraperitoneally (i.p.) administered twice daily (7:00-9:00 a.m. and 7:00-9:00 p.m.) for 8 days. The incidence of spontaneous seizure-induced mortality was observed every morning. |
Dosage form | 2mg/kg; twice a day for 8 days; i.p. |
Applications | SR 57227 hydrochloride treatment prevented spontaneous seizure-induced mortality in mice. |
References: | |
| Cas No. | 77145-61-0 | SDF | |
| 别名 | SR57227盐酸盐 | ||
| 化学名 | 1-(6-chloropyridin-2-yl)piperidin-4-amine hydrochloride | ||
| Canonical SMILES | ClC1=CC=CC(N2CCC(CC2)N)=N1.Cl | ||
| 分子式 | C10H14ClN3.HCl | 分子量 | 248.15 |
| 溶解度 | Soluble to 50 mM in Water and to 100 mM in DMSO | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0298 mL | 20.1491 mL | 40.2982 mL |
| 5 mM | 806 μL | 4.0298 mL | 8.0596 mL |
| 10 mM | 403 μL | 2.0149 mL | 4.0298 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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