A 5-HT2B receptor antagonist
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SB-204741

Item No. 32965

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1-methyl-1H-indol-5-yl)-N′-(3-methyl-5-isothiazolyl)-urea
CAS Number
152239-46-8
Molecular Formula
C14H14N4OS
Formula Weight
286.4
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 15 mg/ml
λmax
231, 270 nm
SMILES
O=C(NC1=CC(C=CN2C)=C2C=C1)NC3=CC(C)=NS3
InChi Code
InChI=1S/C14H14N4OS/c1-9-7-13(20-17-9)16-14(19)15-11-3-4-12-10(8-11)5-6-18(12)2/h3-8H,1-2H3,(H2,15,16,19)
InChi Key
USFUFHFQWXDVMH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $85

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    50 mg

    $337

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    100 mg

    $465

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    Product Description

    SB-204741 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.1 It inhibits 5-HT-induced contraction of isolated rat stomach fundus, a tissue that endogenously expresses high levels of 5-HT2B receptors (pA2 = 7.95). SB-204741 is selective for 5-HT2B receptors over 5-HT1A, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, dopamine D1-3, histamine H1, α1- and α2-adrenergic, and GABAA receptors (Kis = 1-100 µM). In vivo, SB-204741 (1 mg/kg per day) prevents the development of pulmonary arterial hypertension (PAH) and reduces vascular stiffness in a Bmpr2 mutant mouse model of hereditary PAH.2 It also reduces blood pressure in DOCA-salt hypertensive rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Forbes, I.T., Jones, G.E., Murphy, O.E., et al. N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: A novel, high-affinity 5-HT2B receptor antagonist. J. Med. Chem. 38(6), 855-857 (1995).

    2. West, J.D., Carrier, E.J., Bloodworth, N.C., et al. Serotonin 2B receptor antagonism prevents heritable pulmonary arterial hypertension. PLoS One 11(2), e0148657 (2016).

    3. Shingala, J.R., and Balaraman, R. Antihypertensive effect of 5-HT1A agonist buspirone and 5-HT2B antagonists in experimentally induced hypertension in rats. Pharmacology 73(3), 129-139 (2005).