Fluspirilene

Fluspirilene is a dopamine D2 and D3 receptor antagonist (Kis = 1.5 and 1.1 nM, respectively). It is selective for dopamine D2 and D3 receptors over dopamine D1, alpha1- and alpha2-adrenergic, H1 histamine, and sigma-1 (sigma1) receptors (Kis = 450, 102, >5,000, 540, and 150 nM, respectively), muscarinic acetylcholine receptors (mAChRs, Ki = >5,000 nM), and the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, 5-HT2C, and 5-HT3 (Kis = 110, >5,000, 1,830, and >5,000 nM, respectively). Fluspirilene is also a noncompetitive inhibitor of L-type calcium (Cav1) channels with an IC50 value of 30 nM. It inhibits apomorphine-induced vomiting in dogs (ED50 = 0.011 mg/kg). Formulations containing fluspirilene have been used in the treatment of schizophrenia.Formal Name: 8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one. CAS Number: 1841-19-6. Synonyms: McN-JR 6218, R 6218, Redeptin. Molecular Formula: C29H31F2N3O. Formula Weight: 475.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 252, 272, 293 nm. SMILES: FC1=CC=C(C(C2=CC=C(F)C=C2)CCCN3CCC4(C(NCN4C5=CC=CC=C5)=O)CC3)C=C1. InChi Code: InChI=1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35). InChi Key: QOYHHIBFXOOADH-UHFFFAOYSA-N.