Lumateperone (tosylate)

Lumateperone is an atypical antipsychotic. It selectively binds to the serotonin (5-HT) receptor subtype 5-HT2A over 5-HT1A and 5-HT2C receptors (Kis = 0.54, 1,480, and 173 nM, respectively). Lumateperone also binds to dopamine D1, D2, and D4 receptors (Kis = 52, 32, and 108 nM, respectively), alpha1A- and alpha1B-adrenergic receptors (Kis = 73 and 31 nM, respectively), and the 5-HT transporter (SERT, Ki = 61 nM). It reduces head-twitch behavior induced by the 5-HT2A agonist quipazine in rats (ED50 = 0.12 mg/kg). Formulations containing lumateperone have been used in the treatment of schizophrenia.Formal Name: 1-(4-fluorophenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)butan-1-one 4-methylbenzenesulfonic acid. CAS Number: 1187020-80-9. Synonyms: ITI-007. Molecular Formula: C24H28FN3O . C7H8O3S. Formula Weight: 565.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:7): 0.12 mg/ml, DMSO: 10 mg/ml, Ethanol: 1 mg/ml. lambdamax: 229 nm. SMILES: O=S(O)(C1=CC=C(C=C1)C)=O.O=C(C2=CC=C(F)C=C2)CCCN3CC[C@@]4([H])[C@@](C5=CC=CC6=C5N4CCN6C)([H])C3. InChi Code: InChI=1S/C24H28FN3O.C7H8O3S/c1-26-14-15-28-21-11-13-27(16-20(21)19-4-2-5-22(26)24(19)28)12-3-6-23(29)17-7-9-18(25)10-8-17,1-6-2-4-7(5-3-6)11(8,9)10/h2,4-5,7-10,20-21H,3,6,11-16H2,1H3,2-5H,1H3,(H,8,9,10)/t20-,21-,/m0./s1. InChi Key: LHAPOGAFBLSJJQ-GUTACTQSSA-N.