SR 57227 hydrochloride |
Catalog No.GC15630
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Chemical Name | 1-(6-chloropyridin-2-yl)piperidin-4-amine hydrochloride | ||
| Canonical SMILES | ClC1=CC=CC(N2CCC(CC2)N)=N1.Cl | ||
| Formula | C10H14ClN3.HCl | M.Wt | 248.15 |
| Solubility | Soluble to 50 mM in Water and to 100 mM in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)