| Identification | Back Directory | [Name]
PIBOSEROD,2H-(1,3)OXAZINO(3,2-A)INDOLE-10-CARBOXAMIDE, N-((1-BUTYL-4-PIPERIDINYL)METHYL)-3,4-DIHYDRO- | [CAS]
152811-62-6 | [Synonyms]
CS-2135
Sb207256
SB 207266
PIBOSEROD
Piboserod [inn]
Unii-4uq3S81B25
SB207266(Piboserod)
Piboserod(SB-207266)
SB-207266 >=98% (HPLC)
SB-207266;SB 207266;SB207266
N-[(1-Butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide
N-[(1-butylpiperidin-4-yl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide
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- | [Molecular Formula]
C22H31N3O2 | [MDL Number]
MFCD00923681 | [MOL File]
152811-62-6.mol | [Molecular Weight]
369.5 |
| Chemical Properties | Back Directory | [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 | [form ]
powder | [pka]
13.86±0.20(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
Treatment
of irritable bowel syndrome (selective 5HT4receptor
antagonist). | [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 .
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| [IC 50]
5-HT4 Receptor | [storage]
Store at -20°C |
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