PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO-
PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO- Basic information
- Product Name:
- PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO-
- Synonyms:
-
- PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO-
- PIBOSEROD
- Piboserod(SB-207266)
- Piboserod [inn]
- Sb207256
- Unii-4uq3S81B25
- SB 207266
- SB207266(Piboserod)
- CAS:
- 152811-62-6
- MF:
- C22H31N3O2
- MW:
- 369.5
- Product Categories:
-
- Inhibitors
- API
- Mol File:
- 152811-62-6.mol
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PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO- Chemical Properties
- Melting point:
- 110-113°
- Boiling point:
- 570.3±35.0 °C(Predicted)
- Density
- 1.22±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMF: 30 mg/mL; DMSO: 20 mg/mL; Ethanol: 30 mg/mL; Ethanol:PBS (pH7.2)(1:20): 0.05 mg/mL
- pka
- 13.86±0.20(Predicted)
- form
- powder
- color
- white to beige
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PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO- Usage And Synthesis
Uses
Treatment of irritable bowel syndrome (selective 5HT4receptor antagonist).
Uses
Piboserod is a 5-HT4 receptor antagonist which has shown positive results as a Hepatitis C virus (HCV) entry inhibtor.
Biochem/physiol Actions
SB-207266 is a potent, selective, orally active and long-acting 5-HT4 antagonist in vivo.
in vivo
Piboserod (0.3-30mg/kg oral, 0.1mg/kg subcutaneous) can inhibit the gastric fundus contraction response induced by the 5-HT2B receptor agonist BW 723C86 in rat and mouse models, and can also inhibit the esophageal relaxation response induced by the 5-HT4 receptor agonist (such as Tegaserod); in mouse experiments, it can dose-dependently reduce the concentration of SB207145 in the rat striatum, thereby affecting the occupancy of 5-HT4 receptors[3][4].
| Animal Model: | Sprague-Dawley rats (male, 250-350 g), mice models[3][4] |
| Dosage: | 0.3-30 mg/kg for oral administration, 0.1 mg/kg for subcutaneous injection. |
| Administration: | Oral or subcutaneous injection |
| 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 . |
IC 50
5-HT4 Receptor
PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO-Supplier
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