An internal standard for the quantification of brexpiprazole
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Unlabeled Version(s)
22906Brexpiprazole
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Brexpiprazole-d8

Item No. 26450

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A solid
Solubility(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    500 µg

    $290

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    1 mg

    $490

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    Product Description

    Brexpiprazole-d8 is intended for use as an internal standard for the quantification of brexpiprazole (Item No. 22906) by GC- or LC-MS. Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = <1 nM) for 5-HT1A and 5-HT2A serotonin, dopamine D2L, and α1B-, and α2C-adrenergic receptors in CHO cell membranes expressing the human receptors.1 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 α1B- and α2C-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 (Item No. 16094) and amphetamine, and reverses cognitive defects induced by subchronic PCP administration in rats.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maeda, K., Sugino, H., Akazawa, H., et al. Brexpiprazole I: In vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J. Pharmacol. Exp. Ther. 350(3), 589-604 (2014).

    2. Maeda, K., Lerdrup, L., Sugino, H., et al. Brexpiprazole II: Antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulator. J. Pharmacol. Exp. Ther. 350(3), 605-614 (2014).