A selective, potent 5-HT4 receptor antagonist
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SB-207266

Item No. 18778

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1-butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide
CAS Number
152811-62-6
Synonyms
  • Piboserod
Molecular Formula
C22H31N3O2
Formula Weight
369.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 20 mg/mLEthanol: 30 mg/mLEthanol:PBS (pH7.2)(1:20): 0.05 mg/mL
λmax
224, 263, 294 nm
SMILES
CCCCN1CCC(CNC(C2=C3N(CCCO3)C4=C2C=CC=C4)=O)CC1
InChi Code
InChI=1S/C22H31N3O2/c1-2-3-11-24-13-9-17(10-14-24)16-23-21(26)20-18-7-4-5-8-19(18)25-12-6-15-27-22(20)25/h4-5,7-8,17H,2-3,6,9-16H2,1H3,(H,23,26)
InChi Key
KVCSJPATKXABRQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.1,2 In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.3 In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.1,4,5 In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.1 SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wardle, K.A., Bingham, S., Ellis, E.S., et al. Selective and functional 5-hydroxytryptamine4 receptor antagonism by SB 207266. Br. J. Pharmacol. 118(3), 665-670 (1996).

    2. Claeysen, S., Sebben, M., Bécamel, C., et al. Pharmacological properties of 5-Hydroxytryptamine4 receptor antagonists on constitutively active wild-type and mutated receptors. Mol. Pharmacol. 58(1), 136-144 (2000).

    3. Birkeland, J.A.K., Sjaastad, I., Brattelid, T., et al. Effects of treatment with a 5-HT4 receptor antagonist in heart failure. Br. J. Pharmacol. 150(2), 143-152 (2007).