Piboserod
Based on 4 publication(s) in Google Scholar
Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.35%
- CAS. Nr.: 152811-62-6
- Formel: C22H31N3O2
- Molecular Weight:369.50
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Piboserod
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Biologische Aktivität
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5-HT4 Receptor |
Piboserod (1 nM, 100 nM; 30 min) can antagonize the potentiation of 5-HT on the contraction response of bladder detrusor strips induced by electric field stimulation (EFS) in an isolated human bladder detrusor strip experiment in a concentration-dependent manner without changing the basal contraction. The average apparent antagonist dissociation constant KB value is 0.56 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:0.3-30 mg/kg for oral administration, 0.1 mg/kg for subcutaneous injection.
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Administration:Oral or subcutaneous injection
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Result:Attenuated the BW 723C86-mediated contractile responses of the stomach fundus in Sprague-Dawley rats.
Abolished the Tegaserod (0.001-0.3 mg/kg intravenously)-mediated oesophageal relaxation responses in mice.
Dose-dependently decreased the concentrations of SB207145 in the rat striatum, and the effective dose to achieve 50% receptor occupancy with an ED50 of 2.0 mg/kg .
Chemical Information
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CAS. Nr. 152811-62-6
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Appearance Solid
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Molecular Weight 369.50
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Formel C22H31N3O2
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Color White to off-white
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SMILES
O=C(C1=C(OCCC2)N2C3=C1C=CC=C3)NCC4CCN(CCCC)CC4
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Synonyms
SB-207266
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Protein Cell
Identification of serotonin 2A receptor as a novel HCV entry factor by a chemical biology strategy. [Abstract]2019 Mar;10(3):178-195. PMID: 29542010 -
Food Res Int
Polysaccharide from Aloe vera gel improves intestinal stem cells dysfunction to alleviate intestinal barrier damage via 5-HT. [Abstract]2025 Aug:214:116675. PMID: 40467243 -
Neural Regen Res
2023 Sep;18(9):2047-2055. PMID: 36926731 -
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (67.66 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Darblade B, et al. Piboserod (SB 207266), a selective 5-HT4 receptor antagonist, reduces serotonin potentiation of neurally-mediated contractile responses of human detrusor muscle. World J Urol. 2005 Jun;23(2):147-51. [Content Brief]
[2]. Kjekshus JK, et al. Effect of piboserod, a 5-HT4 serotonin receptor antagonist, on left ventricular function in patients with symptomatic heart failure. Eur J Heart Fail. 2009 Aug;11(8):771-8. [Content Brief]
[3]. Nirogi R, et al. In-vivo rat striatal 5-HT4 receptor occupancy using non-radiolabelled SB207145. J Pharm Pharmacol. 2013 May;65(5):704-12. [Content Brief]
[4]. McCullough JL, et al. The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat. Pharmacol Res. 2006 Apr;53(4):353-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.7064 mL | 13.5318 mL | 27.0636 mL | 67.6590 mL |
| 5 mM | 0.5413 mL | 2.7064 mL | 5.4127 mL | 13.5318 mL | |
| 10 mM | 0.2706 mL | 1.3532 mL | 2.7064 mL | 6.7659 mL | |
| 15 mM | 0.1804 mL | 0.9021 mL | 1.8042 mL | 4.5106 mL | |
| 20 mM | 0.1353 mL | 0.6766 mL | 1.3532 mL | 3.3829 mL | |
| 25 mM | 0.1083 mL | 0.5413 mL | 1.0825 mL | 2.7064 mL | |
| 30 mM | 0.0902 mL | 0.4511 mL | 0.9021 mL | 2.2553 mL | |
| 40 mM | 0.0677 mL | 0.3383 mL | 0.6766 mL | 1.6915 mL | |
| 50 mM | 0.0541 mL | 0.2706 mL | 0.5413 mL | 1.3532 mL | |
| 60 mM | 0.0451 mL | 0.2255 mL | 0.4511 mL | 1.1276 mL |
Piboserod Related Classifications
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