| Identification | Back Directory | [Name]
Risperidone (Mesylate) | [CAS]
666179-96-0 | [Synonyms]
Risperidone (Mesylate) APEXIDONE;R-64766;R64766 | [Molecular Formula]
C24H31FN4O5S | [MDL Number]
MFCD28168053 | [MOL File]
666179-96-0.mol | [Molecular Weight]
506.59 |
| Hazard Information | Back Directory | [Uses]
Risperidone mesylate(R 64 766 mesylate) 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. | [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]. | [IC 50]
5-HT2A Receptor: 4.8 nM (Ki); D2 Receptor: 5.9 nM (Ki); P-glycoprotein | [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. DOI:10.1007/BF02251280 [2] Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cellapoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. DOI:10.1016/j.intimp.2011.11.011 [3] Bardgett ME, et al. Adult rats treated with risperidone during development are hyperactive. Exp Clin Psychopharmacol. 2013 Jun;21(3):259-67. DOI:10.1037/a0031972 [4] Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64. DOI:10.1038/sj.npp.1301181 |
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