Brexpiprazole-d8

Brexpiprazole-d8 is intended for use as an internal standard for the quantification of brexpiprazole (Cay-22906) by GC- or LC-MS. Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = 1A and 5-HT2A serotonin, dopamine D2L, and alpha1B-, and alpha2C-adrenergic receptors in CHO cell membranes expressing the human receptors. It acts as a partial agonist of 5-HT1A, D2L, and D3 receptors (EC50s = 0.49, 4.0, and 2.8 nM, respectively) and an antagonist of 5-HT2A, 5-HT2B, as well as alpha1B- and alpha2C-adrenergic receptors (IC50s = 6.5, 14, 0.66, and 63 nM, respectively) in vitro. In vivo, brexpiprazole dose-dependently reduces conditioned avoidance response (CAR) time, inhibits locomoter hyperactivity induced by apomorphine (Cay-16094) and amphetamine, and reverses cognitive defects induced by subchronic PCP administration in rats. It also reduces apomorphine-induced eye blinking in cynomolgus monkeys. Formulations containing brexpiprazole have been used in the treatment of schizophrenia and major depressive disorder.Formal Name: 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl-2,2,3,3,5,5,6,6-d8)butoxy]-2(1H)-quinolinone. CAS Number: 1427049-21-5. Molecular Formula: C25H19D8N3O2S. Formula Weight: 441.6. Purity: >99% deuterated forms (d1-d8). Formulation: (Request formulation change), A solid. Solubility: :, DMSO: soluble. SMILES: O=C1C=CC2=C(C=C(OCCCCN3C([2H])([2H])C([2H])([2H])N(C4=C(C=CS5)C5=CC=C4)C([2H])([2H])C3([2H])[2H])C=C2)N1. InChi Code: InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)/i12D2,13D2,14D2,15D2. InChi Key: ZKIAIYBUSXZPLP-DHNBGMNGSA-N. Origin: Synthetic.