产品介绍
Product Description
Biochem/physiol Actions
Lumateperone tosylate (ITI-007) is an orally active, potent 5-HT2A antagonist, postsynaptic D2 antagonist, and serotonin transporter SERT inhibitor (Ki = 0.5, 32, 62 nM, respectively) with in vivo antipsychotic efficacy and no effect toward receptors associated with cognitive and metabolic side effects of antipsychotic drugs (e.g., H1, 5-HT2C, muscarinic). ITI-007 blocks DOI-induced headtwitch (ID50 = 0.09 mg/kg, po.) and D-AMPH-induced hyperlocomotion in mice (ID50 = 0.95 mg/kg, po.), while also acting as a partial agonist at presynaptic striatal D2 receptors.
Orally active, potent 5-HT2A antagonist, postsynaptic D2 antagonist, and serotonin transporter SERT inhibitor with in vivo antipsychotic efficacy.
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| optical activity | [α]/D -10 to -14, c = 1 in DMSO |
| color | white to very dark gray |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | O=C(C1=CC=C(F)C=C1)CCCN2CC[C@]([C@@]3([H])C2)([H])N4CCN(C)C5=C4C3=CC=C5.O=S(C6=CC=C(C)C=C6)(O)=O |
| 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 |
