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| SKU | Size | Availability |
Price | Qty |
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A408016-1ml
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1ml |
Available within 8-12 weeks(?)
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$134.90
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5-HT1 Selective Inhibitors | Agonists | Antagonists | Modulators
| Synonyms | OPC-14597 | 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone |
|---|---|
| Specifications & Purity | Moligand™, 10mM in DMSO |
| Biochemical and Physiological Mechanisms | Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist. |
| Storage Temp | Store at -80°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Grade | Moligand™ |
| Action Type | AGONIST, ANTAGONIST, PARTIAL AGONIST |
| Mechanism of action | Serotonin 2a (5-HT2a) receptor antagonist |
| Product Description |
Information Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity5-HT receptorpartial agonist. Aripiprazole binds with high affinity to both the G protein-coupled and uncoupled states of receptors. Aripiprazole potently activates D2 receptor-mediated inhibition of cAMP accumulation. Aripiprazole has highest affinity for h5-HT(2B)-, hD(2L)-, and hD(3)-dopamine receptors, but also has significant affinity (5-30 nM) for several other 5-HT receptors (5-HT(1A), 5-HT(2A), 5-HT(7)), as well as alpha(1A)-adrenergic and hH(1)-histamine receptors. Aripiprazole has less affinity (30-200 nM) for other G protein-coupled receptors, including the 5-HT(1D), 5-HT(2C), alpha(1B)-, alpha(2A)-, alpha(2B)-, alpha(2C)-, beta(1)-, and beta(2)-adrenergic, and H(3)-histamine receptors. Aripiprazole is an inverse agonist at 5-HT(2B) receptors and displays partial agonist actions at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors. In vivo Aripiprazole reduces extracellular 5-HIAA concentrations in the medial prefrontal cortex and striatum of drug-naive rats, but not in chronic Aripiprazole-pretreated rats. Aripiprazole, 0.1 mg/kg and 0.3 mg/kg, significantly increases dopamine release in the hippocampus of rats. Aripiprazole, 0.3 mg/kg, slightly but significantly increases dopamine release in the medial prefrontal cortex but not in the nucleus accumbens. Aripiprazole, 3.0 mg/kg and 10 mg/kg, significantly decreases dopamine release in the nucleus accumbens but not the medical prefrontal cortex. Aripiprazole, 0.3 mg/kg, transiently potentiates haloperidol (0.1 mg/kg)-induced dopamine release in the medial prefrontal cortex but inhibited that in the nucleus accumbens. cell lines: Concentrations: Incubation Time: Powder Purity:≥98% |
| Ki Data | 5-HT1A, Ki: 4.2 nM |
|---|---|
| ALogP | 4.998 |
| hba_count | 2 |
| HBD Count | 1 |
| Rotatable Bond | 7 |
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| Smiles | ClC1=CC=CC(=C1Cl)N2CCN(CCCCOC3=CC=C4CCC(=O)NC4=C3)CC2 |
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| Molecular Weight | 448.39 |
| Reaxy-Rn | 7951706 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7951706&ln= |
| Solubility | Solubility (25°C) In vitro DMSO: 37 mg/mL (198.65 mM); |
|---|---|
| DMSO(mg / mL) Max Solubility | 90 |
| DMSO(mM) Max Solubility | 200.72 |
| Water(mg / mL) Max Solubility | <1 |
| 1. Huanhuan Yang, Cong Liu, Chuanhong Zhu, Yan Zheng, Juan Li, Qianyun Zhu, Hao Wang, Xiangming Fang, Quan Liu, Man Liang, Zilong Liu. (2023) Determination of ten antipsychotics in blood, hair and nails: Validation of a LC–MS/MS method and forensic application of keratinized matrix analysis. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 234 (115557). |