Formulation: A solid
Formal Name: 3,5-dihydro-5-methyl-N-3-pyridinyl-benzo[1,2-b:4,5-b′]dipyrrole-1(2H)-carboxamide, monohydrochloride
Purity: ≥98%
Formula Markup: C17H16N4O • HCl
Formula Weight: 328,8
Shelf life (days): 1460
CAS Number: 1197334-04-5
Notes: SB-206553 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 12.6 nM) and 5-HT2B.{63059} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT3, 5-HT4, and 5-HT7 receptors, as well as dopamine D2, D3, and D4, α1-adrenergic, histamine H1, and adenosine A1 receptors (Kis = >1 µM for all). SB-206553 inhibits 5-HT-induced contraction of isolated rat stomach fundus, a tissue rich in 5-HT2B receptors, with an EC50 value of 4.8 nM. It inhibits 5-HT-induced inositol phosphate release in HEK293 cells expressing human 5-HT2C receptors (EC50 = 3.16 nM). SB-206553 (2 and 20 mg/kg) increases the time spent in active social interaction in a social interaction test and increases punished responding in the Geller-Seifter conflict test in rats, indicating anxiolytic-like activity. It also increases suppressed responding in a marmoset conflict model of anxiety when administered at doses of 15 and 20 mg/kg.
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