A serotonin and dopamine receptor modulator
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Labeled Version(s)
26450Brexpiprazole-d8
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Brexpiprazole

Item No. 22906

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]-2(1H)-quinolinone
CAS Number
913611-97-9
Synonyms
  • OPC 34712
Molecular Formula
C25H27N3O2S
Formula Weight
433.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:7): 0.1 mg/mlDMSO: 25 mg/mlEthanol: 1 mg/ml
λmax
215 nm
SMILES
O=C1C=CC2=C(C=C(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)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)
InChi Key
ZKIAIYBUSXZPLP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    10 mg

    $49

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    50 mg

    $143

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    100 mg

    $259

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    Product Description

    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).