SB-206553 (hydrochloride)

SB-206553 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 12.6 nM) and 5-HT2B. 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, alpha1-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.Formal Name: 3,5-dihydro-5-methyl-N-3-pyridinyl-benzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide, monohydrochloride. CAS Number: 1197334-04-5. Molecular Formula: C17H16N4O . HCl. Formula Weight: 328.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 214, 236, 272, 325 nm. SMILES: O=C(N1C2=CC3=C(C=C2CC1)N(C)C=C3)NC4=CN=CC=C4.Cl. InChi Code: InChI=1S/C17H16N4O.ClH/c1-20-7-4-12-10-16-13(9-15(12)20)5-8-21(16)17(22)19-14-3-2-6-18-11-14,/h2-4,6-7,9-11H,5,8H2,1H3,(H,19,22),1H. InChi Key: VGEMBOFBPSNOIO-UHFFFAOYSA-N.