Ritanserin

Ritanserin is a selective antagonist of the serotonin (5-HT) receptor subtype, 5-HT2A. In a radioligand binding assay, ritanserin exhibits high selectivity for 5-HT2A over 5-HT1 receptors (IC50s = 0.9 nM and >1000 nM, respectively). It also demonstrates relatively low affinity for histamine H1, dopamine D2, alpha1-adrenergic, and alpha2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). Ritanserin (2.5 mg/kg) is long-acting, occupying >70% of 5-HT2A sites up to 48 hours following subcutaneous administration to rats and guinea pigs. In vivo, ritanserin (10 mg/kg) blocks 5-hydroxy tryptophan-induced head twitches in rats.Formal Name: 6-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one. CAS Number: 87051-43-2. Synonyms: R-55-667. Molecular Formula: C27H25F2N3OS. Formula Weight: 477.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 12.5 mg/ml, Ethanol: 2.5 mg/ml. lambdamax: 229, 324 nm. SMILES: FC1=CC=C(/C(C2=CC=C(F)C=C2)=C3CCN(CCC4=C(C)N=C(SC=C5)N5C4=O)CC\3)C=C1. InChi Code: InChI=1S/C27H25F2N3OS/c1-18-24(26(33)32-16-17-34-27(32)30-18)12-15-31-13-10-21(11-14-31)25(19-2-6-22(28)7-3-19)20-4-8-23(29)9-5-20/h2-9,16-17H,10-15H2,1H3. InChi Key: JUQLTPCYUFPYKE-UHFFFAOYSA-N.