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Aripiprazole - 10mM in DMSO, high purity , CAS No.129722-12-9(DMSO), Serotonin 2a (5-HT2a) receptor antagonist

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Item Number
A408016
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A408016-1ml
1ml
Available within 8-12 weeks(?)
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$134.90

5-HT1 Selective Inhibitors | Agonists | Antagonists | Modulators

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Compound libraries (12325)

Basic Description

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.
In vitro

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 Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥98%

Product Properties

Ki Data 5-HT1A, Ki: 4.2 nM
ALogP 4.998
hba_count 2
HBD Count 1
Rotatable Bond 7

Associated Targets(Human)

DRD2 Tclin D(2) dopamine receptor (58 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
DRD4 Tchem D(4) dopamine receptor (10 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABCB1 Tchem Multidrug resistance protein 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HRH1 Tclin Histamine H1 receptor (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
SLC6A4 Tclin Sodium-dependent serotonin transporter (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
DRD3 Tclin D(3) dopamine receptor (25 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR1B Tclin 5-hydroxytryptamine receptor 1B (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA2C Tclin Alpha-2C adrenergic receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR2A Tclin 5-hydroxytryptamine receptor 2A (24 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR7 Tclin 5-hydroxytryptamine receptor 7 (9 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA1B Tclin Alpha-1B adrenergic receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA2A Tclin Alpha-2A adrenergic receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA1A Tclin Alpha-1A adrenergic receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR1D Tclin 5-hydroxytryptamine receptor 1D (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR2C Tclin 5-hydroxytryptamine receptor 2C (7 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR1A Tclin 5-hydroxytryptamine receptor 1A (18 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR3A Tclin 5-hydroxytryptamine receptor 3A (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR6 Tchem 5-hydroxytryptamine receptor 6 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR2B Tclin 5-hydroxytryptamine receptor 2B (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
H1F0 Tchem Histone H1.0 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (8 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles ClC1=CC=CC(=C1Cl)N2CCN(CCCCOC3=CC=C4CCC(=O)NC4=C3)CC2
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=

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

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

Citations of This Product

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). 

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