CAS Number106266-06-2
SynonymsRispadal; Psychodal; MFCD00274576; Belivon; Risperidal; Kesperidone; Risperdal; Spiron; Risperidone; Apexidone; R 64 766,Risperdal; R 64,766,Risperidone
Molecular FormulaC23H27FN4O2
Molecular Weight410.48
Purity≥98 (HPLC)%
Density1.4±0.1 g/cm3
Boiling Point572.4±60.0 °C at 760 mmHg
Melting Point170°C
Appearancepowder
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 106266-06-2 |
| Catalog No. | 2A-9012316 |
| Chinese Name | 利培酮 |
| Synonyms | Rispadal; Psychodal; MFCD00274576; Belivon; Risperidal; Kesperidone; Risperdal; Spiron; Risperidone; Apexidone; R 64 766,Risperdal; R 64,766,Risperidone |
| Molecular Formula | C23H27FN4O2 |
| Molecular Weight | 410.48 |
| Purity | ≥98 (HPLC) |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 572.4±60.0 °C at 760 mmHg |
| Melting Point | 170°C |
| Appearance | powder |
| Storage Condition | Store sealed and in a cool, dry warehouse. |
| Packaging | II |
| Application | Risperidone is a 5-HT2 receptor blocker, a P-glycoprotein inhibitor and a dopamine D2 receptor antagonist. Its Ki values for 5-HT2A and dopamine D2 receptors are 4.8 and 5.9 nM respectively. |
| HTC | 2934999090 |
| PubChem ID | 329824020 |
| MDL Number | MFCD00274576 |
| SMILES | CC1=C(CCN2CCC(CC2)c3noc4cc(F)ccc34)C(=O)N5CCCCC5=N1 |
| InChI | 1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3 |
| InChI Key | RAPZEAPATHNIPO-UHFFFAOYSA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| Hazard Symbols | 6.1(a) |
| MSDS | msds/12316_1_106266_06_2.pdf |
| Bioactivity | Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively. Related Catalog Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Neurological Disease Target 5-HT2A Receptor:4.8 nM (Ki) dopamine D2 receptor:5.9 nM (Ki) P-Glycoprotein In Vitro Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively. Risperidone dose-dependently inhibited the release of IL-12 in mature DCs, while the production of IL-10 is dose-dependently increased by Risperidone. A high dose of risperidone can induce TNF-α release from mature DCs[3]. In Vivo In the first experiment, body weight is found to be slightly but significantly lower in the Risperidone-treated rats as a function of age. Similar to the first experiment, age-dependent differences in body weight are also observed between the three treatment groups in the second locomotor experiment. Rats treated with the 3.0 mg/kg dose of Risperidone weigh less than vehicle-treated rats on postnatal days 35, 38, and 41. The third locomotor experiment involves larger, mixed-sex litters in contrast to the smaller, single-sex litters used in the first two experiments. As noted for the first two experiments, rats treated with Risperidone in the third experiment gain less weight in an age-dependent manner[4]. Animal Admin Rats[4] A total of 211 Long-Evans rats (56 females and 155 males) are used. Within each study, three groups of roughly equal numbers of rats receive injections of 1.0 mg/kg of Risperidone, 3.0 mg/kg of Risperidone, or the vehicle used for the Risperidone solution as a control. In the first experiment, twenty-six male rats (n=9 in the vehicle and 3.0 mg/kg Risperidone groups; n=8 in the 1.0 mg/kg Risperidone group) are tested for locomotor activity for 20 minutes a day beginning at postnatal day 49 and continuing daily until postnatal day 53. A second experiment determined if the locomotor effects of early-life Risperidone treatment persisted well into adulthood. A third experiment ascertains the effects of sex on the locomotor effects of early-life Risperidone seen in young adult rats. In this experiment, sixty male (n=20 per treatment group) and 56 female (n=19 rats in the vehicle and 3.0 mg/kg dose group, n=18 in the 1.0 mg/kg dose group) rats are treated. A fourth experiment assessed reversal learning during adulthood in rats administered earlylife risperidone. Forty-two male rats (n=14 per treatment group) are treated[4]. References [1]. Nyberg S, et al. 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology (Berl). 1993;110(3):265-72. [2]. Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64. [3]. Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cell apoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. [4]. Bardgett ME, et al. Adult rats treated with risperidone during development are hyperactive. Exp Clin Psychopharmacol. 2013 Jun;21(3):259-67. Chemical & Physical Properties Density 1.4±0.1 g/cm3 Boiling Point 572.4±60.0 °C at 760 mmHg Melting Point 170°C Molecular Formula C23H27FN4O2 Molecular Weight 410.484 Flash Point 300.0±32.9 °C Exact Mass 410.211792 PSA 64.16000 LogP 2.88 Vapour Pressure 0.0±1.6 mmHg at 25°C Index of Refraction 1.677 InChIKey RAPZEAPATHNIPO-UHFFFAOYSA-N SMILES Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2 Storage condition Room temp |
| Use of | Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively. Properties Articles125 Name risperidone Synonym More Synonyms Risperidone Biological Activity Description Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively. Related Catalog Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Neurological Disease 5-HT2A Receptor:4.8 nM (Ki) dopamine D2 receptor:5.9 nM (Ki) P-Glycoprotein In Vitro Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively. Risperidone dose-dependently inhibited the release of IL-12 in mature DCs, while the production of IL-10 is dose-dependently increased by Risperidone. A high dose of risperidone can induce TNF-α release from mature DCs[3]. References [1]. Nyberg S, et al. 5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology (Berl). 1993;110(3):265-72. [2]. Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64. [3]. Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cell apoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. [4]. Bardgett ME, et al. Adult rats treated with risperidone during development are hyperactive. Exp Clin Psychopharmacol. 2013 Jun;21(3):259-67. Chemical & Physical Properties Molecular Formula C23H27FN4O2 Exact Mass 410.211792 PSA 64.16000 Index of Refraction 1.677 InChIKey RAPZEAPATHNIPO-UHFFFAOYSA-N Storage condition Room temp |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Shipping Name: UN |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN dangerous goods number European Dangerous Regulations for land transport: 2811 International Dangerous Regulations for sea transport: 2811 International Dangerous Regulations for air transport: 2811 14.2 United Nations shipping name European Land Transport Dangerous Regulations: TOXIC SOLID, ORGANIC, N.O.S. (Risperidone) IMDG: TOXIC SOLID, ORGANIC, N.O.S. (Risperidone) International air transport hazard regulations: Toxic solid, organic, n.o.s. (Risperidone) 14.3 Transport hazard categories European Land Transport Danger Regulations: 6.1 International Maritime Transport Danger Regulations: 6.1 International Air Transport Danger Regulations: 6.1 14.4 Package group European Land Transport Danger Regulations: III International Maritime Transport Danger Regulations: III International Air Transport Danger Regulations: III 14.5 Environmental hazards European Land Transport Danger Regulations: No International Maritime Danger Regulations International Air Transport Danger Regulations: No Marine pollutants (yes/no): No 14.6 Special reminder to users No data available The above information is believed to be correct, but is not all-inclusive and should be used as a guide only. The information in this document is based on our current knowledge and is Correct safety instructions apply to this product. This information does not represent a warranty as to the properties of this product. See reverse side of invoice or packing slip. |
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