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Brexpiprazole dihydrochloride
- OPC 34712 dihydrochloride
- Parent CAS: 913611-97-9
- Soluble in DMSO
- MF: C25H27N3O2S.2HCl
- MW: 506.49
Description
Brexpiprazole dihydrochloride (OPC-34712) is a serotonin-dopamine activity modulator with high affinity for h5-HT1A, h5-HT2A, hD2L, hα1B and hα2C receptors, each reported with Ki values below 1 nM. It acts as a partial agonist at 5-HT1A and D2 receptors and as an antagonist at 5-HT2A and adrenergic receptor subtypes.
Balanced dopaminergic, serotonergic and adrenergic receptor modulation is relevant to antipsychotic and mood-disorder pharmacology. Brexpiprazole dihydrochloride is useful for profiling atypical antipsychotic mechanisms and multi-receptor CNS pharmacology.
Key Features
- High-affinity serotonin-dopamine activity modulator
- Ki values <1 nM at 5-HT1A, 5-HT2A, D2L, α1B and α2C receptors
- Partial agonist at 5-HT1A and D2 receptors
- Antagonist at 5-HT2A and adrenergic receptors
Applications
- Antipsychotic mechanism research
- Dopamine and serotonin receptor pharmacology
- CNS multi-target profiling
- Neuropsychiatric disease model studies
More Information
| Parent CAS No. | 913611-97-9 |
|---|---|
| Chemical Name | 7-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one dihydrochloride |
| SMILES | N1C2=C(C=CC(OCCCCN3CCN(C4=C5C=CSC5=CC=C4)CC3)=C2)C=CC1=O.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C25H27N3O2S.2ClH/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);2*1H |
| InChiKey | XFZHLEXUSDOLPT-UHFFFAOYSA-N |
| CID | 91826510 |
| Short Description | Antipsychotic |
References
- K. Maeda et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604.
- K. Maeda et al. Brexpiprazole II: antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):605-14.
- N. Yoshimi et al. Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors. Pharmacol Biochem Behav. 2014 Sep;124:245-9.
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