SB-204741

SB-204741

CAT N°: 32965
Price:

From 211.00 179.35

SB-204741 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.{61368} 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, ?1- and ?2-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.{61369} It also reduces blood pressure in DOCA-salt hypertensive rats.{61370}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-(1-methyl-1H-indol-5-yl)-N?-(3-methyl-5-isothiazolyl)-urea
  • Correlated keywords
    • SB204741 5HT 2B 1A 1D 1E 2A 2C 3 4 5HT2B 5HT1A 5HT1D 5HT1E 5HT2A 5HT2C 5HT3 5HT4 GABA A Bmpr 2
  • Product Overview:
    SB-204741 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.{61368} 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, ?1- and ?2-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.{61369} It also reduces blood pressure in DOCA-salt hypertensive rats.{61370}

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