Risperidone - Moligand™, 2mM in DMSO , Dopamine D2 receptor antagonist, CAS No.106266-06-2, Dopamine D2 receptor antagonist

CAS: 106266-06-2 Cat. No.: R409182 分子式: C₂₃H₂₇FN₄O₂ 分子量: 410.48 EC番号: 600-733-1 PubChem CID: 5073

GRADE & PURITY Moligand™, 2mM in DMSO

Synonyms

R-64766 | 3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

Risperidone (R-64766) is a mutil-targeted antagonist fordopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.
In vitro

Risperidone\xa0binds to both DA and serotonin (5HT) receptors, particularly in the neurons of striatal and limbic structures. Risperidone significantly affects brain nerve growth factor (NGF) level suggesting that it influences the turnover of endogenous growth factors. Risperidone\xa0significantly decreases BDNF concentrations in frontal cortex, occipital cortex and hippocampus and decreases or increases TrkB receptors in selected\xa0brain\xa0structures. Risperidone significantly increases D(2) binding in medial prefrontal cortex\xa0by 34%\xa0in\xa0rat\xa0forebrain\xa0regions. Risperidone produces even greater up-regulation of D(4) receptors in CPu (37%), NAc (32%), and HIP (37%) in\xa0rat\xa0forebrain\xa0regions. Risperidone\xa0significantly inhibits the production of NO and proinflammatory cytokines by activated microglia. Risperidone (1-50 mM) significantly enhances the intracellular accumulation of Rh123 in Caco-2 cells by inhibiting P-gp\xa0activity\xa0with an IC(50) value of 5.87 mM.

In vivo

Risperidone does not significantly affect bodyweight\xa0gain (BWG), food intake(FI),\xa0glucose\xa0tolerance\xa0or leptin levels, even though prolactin and corticosterone are significantly elevated in male rats. Risperidone significantly increases BWG and FI in female rats. Risperidone (0.05 mg/kg) increases food intake and leptin gene expression in white adipose tissue (WAT), but the rate of\xa0bodyweight\xa0gain\xa0is not affected in rats.\xa0Risperidone (0.5 mg/kg) causes a reduction in\xa0bodyweight\xa0gain, as well as enhanced Ucp1 gene expression in BAT and serum prolactin concentrations in rats.
Cell Data

cell lines：HCT116

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

同義語

R-64766 | 3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

仕様と純度

Moligand™, 2mM in DMSO

生化学的・生理学的メカニズム

Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

ANTAGONIST

作用メカニズム

Dopamine D2 receptor antagonist

製品の性質

• ALogP: 2.7

名前と識別子

• 異性体SMILES: CC1=C(C(=O)N2CCCCC2=N1)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
• WGKドイツ: 3
• RTECS: UV1164800
• PubChem CID: 5073
• UN番号: 2811
• 包装グループ: III
• 分子量: 410.48
• Reaxy-Rn: 4891881

関連ターゲット（人間）

DRD1 Tclin D(1A) dopamine receptor (1 Activities)

Discover Target: DRD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor (22 Activities)

Discover Target: DRD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD4 Tchem D(4) dopamine receptor (7 Activities)

Discover Target: DRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor (10 Activities)

Discover Target: HRH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter (1 Activities)

Discover Target: SLC6A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor (14 Activities)

Discover Target: DRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1B Tclin 5-hydroxytryptamine receptor 1B (1 Activities)

Discover Target: HTR1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor (2 Activities)

Discover Target: ADRA2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor (4 Activities)

Discover Target: ADRA2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A (24 Activities)

Discover Target: HTR2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1E Tchem 5-hydroxytryptamine receptor 1E (1 Activities)

Discover Target: HTR1E

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR7 Tclin 5-hydroxytryptamine receptor 7 (4 Activities)

Discover Target: HTR7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1B Tclin Alpha-1B adrenergic receptor (2 Activities)

Discover Target: ADRA1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor (4 Activities)

Discover Target: ADRA2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1D Tclin Alpha-1D adrenergic receptor (3 Activities)

Discover Target: ADRA1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor (10 Activities)

Discover Target: ADRA1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1F Tclin 5-hydroxytryptamine receptor 1F (1 Activities)

Discover Target: HTR1F

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C (24 Activities)

Discover Target: HTR2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A (2 Activities)

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR6 Tchem 5-hydroxytryptamine receptor 6 (1 Activities)

Discover Target: HTR6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B (3 Activities)

Discover Target: HTR2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

H1F0 Tchem Histone H1.0 (1 Activities)

Discover Target: H1F0

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GLRA1 Tclin Glycine receptor subunit alpha-1 (1 Activities)

Discover Target: GLRA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (22 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 37 mg/mL (200.82 mM); Ethanol: -1 mg/mL
• 融点（°C）: 172 °C

参考文献

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,      [PMID:37406464] [10.1016/j.jpba.2023.115557]

2. Chao Hao, Changping Fan, Lanting Gao, Mingyue Yin, Xue Jiang, Chenchen Wang, Xingyin Wang, Chaoyang Yin, Guisen Zhang, Jian Zhang.  (2025)  Sustained dissolution and pharmacokinetics of risperidone microsuspensions via cocrystallization with kaempferol.  JOURNAL OF MOLECULAR STRUCTURE,      [PMID:] [10.1016/j.molstruc.2025.143303]