Risperidone Inhibitor CAS No. 106266-06-2

Cat. No.	Name	Size	Price
KI0839	Risperidone	10 mg	$112
	Risperidone	50 mg	$432
	Risperidone	200 mg	$1232

Chemical Characteristic

Product Name	Risperidone
CAS No.	106266-06-2
Molecular Weight	410.48
Formula	C₂₃H₂₇FN₄O₂
Chemical Structure

Biological activities

Risperidone is a dopamine and 5-HT receptors inhibitor. Risperidone inhibits dopamine-2 (D_{2), serotonin-2C (5-HT_{2C), dopamine-4 (D_{4), and dopamine-1 (D_{11) receptors with IC50 of 4, 48, 7 and 50 nM, respectively.^[1] Risperidone inhibits serotonin 5-HT_{2 receptor with a Ki of 0.16 nM. Risperidone is also a potent dopamine D_{2 receptor antagonist with a Ki of 1.4 nM. Risperidone shows all effects common to D_{2 antagonists, including enhancement of prolactin release.^[2] Risperidone is one of the most commonly used atypical antipsychotics and its major route of elimination is oxidation via hepatic CYP2D6 to 9-hydroxy-risperidone (PALI). Risperidone and its major active metabolite are substrates of the drug transporter P-glycoprotein (P-gp). The IC50 of risperidone for inhibiting P-gp-mediated transport of Rh123 and DOX are 63.26 and 15.78µM, respectively. The Ki for binding to the 5HT_{2A receptor subtype for risperidone is 0.16 nM.^[3] In vivo, risperidone inhibits peripherally and centrally 5-HT_{2 receptor agonists in rats with ED50 of 1.1 and 14 µg/kg, respectively. ^[2]}}}}}}}}}

References

[1] Krystal JH, et al. Toward a rational pharmacotherapy of comorbid substance abuse in schizophrenic patients. Schizophr Res. 1999, 35: 35-49. 閵嗏偓閵嗏偓 [2] Megens AA, et al. Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology. 1994, 114: 9-23. [3] Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007, 32(4): 757-764. 閵嗏偓閵嗏偓

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