Risperidone
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MedKoo CAT#: 318669

CAS#: 106266-06-2 (free base)

Description: Risperidone is an antipsychotic medication. It is mainly used to treat schizophrenia, bipolar disorder, and irritability in people with autism. It is taken either by mouth or by injection into a muscle.


Chemical Structure

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Risperidone
CAS# 106266-06-2 (free base)

Theoretical Analysis

MedKoo Cat#: 318669
Name: Risperidone
CAS#: 106266-06-2 (free base)
Chemical Formula: C23H27FN4O2
Exact Mass: 410.21
Molecular Weight: 410.485
Elemental Analysis: C, 67.30; H, 6.63; F, 4.63; N, 13.65; O, 7.80

Price and Availability

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50mg USD 350 Ready to ship
200mg USD 550 Ready to ship
500mg USD 750 Ready to ship
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Related CAS #: 666179-96-0 (mesylate)   106266-06-2 (free base)    

Synonym: Risperidone, Risperidal, R 64766; R-64766, R64766

IUPAC/Chemical Name: 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

InChi Key: RAPZEAPATHNIPO-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=C1C(CCN2CCC(C3=NOC4=CC(F)=CC=C34)CC2)=C(C)N=C5N1CCCC5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: 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.
In vitro activity: In addition, individual treatment with Risperidone brought about promotion of OPG mRNA and protein expression and inhibition of collagen I and RANKL mRNA and protein expression levels, the effect of which was abolished by additional TNF-α silencing. Meanwhile, additional SATB2 silencing also induced the promotion of OPG expression and inhibition of collagen I and RANKL expression levels in the Risperidone-treated TNF-α-deficient MC3T3-E1 cells (Fig. 5A, B, Additional file 1: Fig. S1A). Reference: Mol Med. 2022 May 3;28(1):46. https://pubmed.ncbi.nlm.nih.gov/35505281/
In vivo activity: In contrast, in risperidone-treated rats, the immunoreactivity of the pro-inflammatory cytokines was significantly decreased, and the anti-inflammatory cytokines were enhanced compared to vehicle-treated rats. In brief, risperidone treatment after ACA/CPR (asphyxia CA and cardiopulmonary resuscitation) in rats significantly improved the survival rate and attenuated paralysis, the damage/death (loss) of motor neurons, and inflammation in the lumbar anterior horn. Thus, risperidone might be a therapeutic agent for paraplegia by attenuation of the damage/death (loss) of spinal motor neurons and neuroinflammation after ACA/CPR. Reference: Vet Sci. 2021 Oct 13;8(10):230. https://pubmed.ncbi.nlm.nih.gov/34679060/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 0.1 0.24
DMF:PBS (pH 7.2) (1:1) 0.5 1.22
DMSO 4.8 11.63
Ethanol 2.8 6.82

Preparing Stock Solutions

The following data is based on the product molecular weight 410.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Zhang S, He W, Li A, Zhao C, Chen Y, Xu C, Zhang Q, Zheng D, Chen M, Miao H, Huang Y. Involvement of the TNF-α/SATB2 axis in the induced apoptosis and inhibited autophagy of osteoblasts by the antipsychotic Risperidone. Mol Med. 2022 May 3;28(1):46. doi: 10.1186/s10020-022-00466-9. PMID: 35505281; PMCID: PMC9066868. 2. Canfrán-Duque A, Pastor Ó, García-Seisdedos D, Molina YL, Babiy B, Lerma M, Sánchez-Castellano C, Martínez-Botas J, Gómez-Coronado D, Lasunción MA, Cruz-Jentoft AJ, Busto R. The Antipsychotic Risperidone Alters Dihydroceramide and Ceramide Composition and Plasma Membrane Function in Leukocytes In Vitro and In Vivo. Int J Mol Sci. 2021 Apr 10;22(8):3919. doi: 10.3390/ijms22083919. PMID: 33920193; PMCID: PMC8069118. 3. Rami FZ, Nguyen TB, Oh YE, Karamikheirabad M, Le TH, Chung YC. Risperidone Induced DNA Methylation Changes in Dopamine Receptor and Stathmin Genes in Mice Exposed to Social Defeat Stress. Clin Psychopharmacol Neurosci. 2022 May 31;20(2):373-388. doi: 10.9758/cpn.2022.20.2.373. PMID: 35466108; PMCID: PMC9048015. 4. Lee TK, Lee JC, Tae HJ, Kim HI, Shin MC, Ahn JH, Park JH, Kim DW, Hong S, Choi SY, Cho JH, Won MH. Therapeutic Effects of Risperidone against Spinal Cord Injury in a Rat Model of Asphyxial Cardiac Arrest: A Focus on Body Temperature, Paraplegia, Motor Neuron Damage, and Neuroinflammation. Vet Sci. 2021 Oct 13;8(10):230. doi: 10.3390/vetsci8100230. PMID: 34679060; PMCID: PMC8537088.
In vitro protocol: 1. Zhang S, He W, Li A, Zhao C, Chen Y, Xu C, Zhang Q, Zheng D, Chen M, Miao H, Huang Y. Involvement of the TNF-α/SATB2 axis in the induced apoptosis and inhibited autophagy of osteoblasts by the antipsychotic Risperidone. Mol Med. 2022 May 3;28(1):46. doi: 10.1186/s10020-022-00466-9. PMID: 35505281; PMCID: PMC9066868. 2. Canfrán-Duque A, Pastor Ó, García-Seisdedos D, Molina YL, Babiy B, Lerma M, Sánchez-Castellano C, Martínez-Botas J, Gómez-Coronado D, Lasunción MA, Cruz-Jentoft AJ, Busto R. The Antipsychotic Risperidone Alters Dihydroceramide and Ceramide Composition and Plasma Membrane Function in Leukocytes In Vitro and In Vivo. Int J Mol Sci. 2021 Apr 10;22(8):3919. doi: 10.3390/ijms22083919. PMID: 33920193; PMCID: PMC8069118
In vivo protocol: 1. Rami FZ, Nguyen TB, Oh YE, Karamikheirabad M, Le TH, Chung YC. Risperidone Induced DNA Methylation Changes in Dopamine Receptor and Stathmin Genes in Mice Exposed to Social Defeat Stress. Clin Psychopharmacol Neurosci. 2022 May 31;20(2):373-388. doi: 10.9758/cpn.2022.20.2.373. PMID: 35466108; PMCID: PMC9048015. 2. Lee TK, Lee JC, Tae HJ, Kim HI, Shin MC, Ahn JH, Park JH, Kim DW, Hong S, Choi SY, Cho JH, Won MH. Therapeutic Effects of Risperidone against Spinal Cord Injury in a Rat Model of Asphyxial Cardiac Arrest: A Focus on Body Temperature, Paraplegia, Motor Neuron Damage, and Neuroinflammation. Vet Sci. 2021 Oct 13;8(10):230. doi: 10.3390/vetsci8100230. PMID: 34679060; PMCID: PMC8537088.

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1: Sampson S, Hosalli P, Furtado VA, Davis JM. Risperidone (depot) for schizophrenia. Cochrane Database Syst Rev. 2016 Apr 14;4:CD004161. [Epub ahead of print] Review. PubMed PMID: 27078222.

2: Corena-McLeod M. Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. Review. PubMed PMID: 25943458; PubMed Central PMCID: PMC4488186.

3: Ennis ZN, Damkier P. Pregnancy exposure to olanzapine, quetiapine, risperidone, aripiprazole and risk of congenital malformations. A systematic review. Basic Clin Pharmacol Toxicol. 2015 Apr;116(4):315-20. doi: 10.1111/bcpt.12372. Epub 2015 Jan 28. Review. PubMed PMID: 25536446.

4: Dinnissen M, Dietrich A, van den Hoofdakker BJ, Hoekstra PJ. Clinical and pharmacokinetic evaluation of risperidone for the management of autism spectrum disorder. Expert Opin Drug Metab Toxicol. 2015 Jan;11(1):111-24. doi: 10.1517/17425255.2015.981151. Epub 2014 Nov 11. Review. PubMed PMID: 25385293.

5: Perera MA, Yogaratnam J. De Novo delayed onset hypothermia secondary to therapeutic doses of risperidone in bipolar affective disorder. Ther Adv Psychopharmacol. 2014 Apr;4(2):70-4. doi: 10.1177/2045125313507740. Review. PubMed PMID: 24688758; PubMed Central PMCID: PMC3952484.

6: Tsermpini EE, Assimakopoulos K, Bartsakoulia M, Iconomou G, Papadima EM, Mitropoulos K, Squassina A, Patrinos GP. Individualizing clozapine and risperidone treatment for schizophrenia patients. Pharmacogenomics. 2014 Jan;15(1):95-110. doi: 10.2217/pgs.13.219. Review. PubMed PMID: 24329194.

7: Ghanizadeh A. Evidence based administration of risperidone and paliperidone for the treating conduct disorder. J Res Med Sci. 2013 Nov;18(11):998-1003. Review. PubMed PMID: 24523788; PubMed Central PMCID: PMC3906794.

8: Vieweg WV, Hasnain M, Hancox JC, Baranchuk A, Digby GC, Kogut C, Crouse EL, Koneru JN, Deshmukh A, Pandurangi AK. Risperidone, QTc interval prolongation, and torsade de pointes: a systematic review of case reports. Psychopharmacology (Berl). 2013 Aug;228(4):515-24. doi: 10.1007/s00213-013-3192-8. Epub 2013 Jun 30. Review. PubMed PMID: 23812796.

9: Takeuchi K, Sanjo K, Sakai A. [Paliperidone, risperidone]. Nihon Rinsho. 2013 Apr;71(4):654-9. Review. Japanese. PubMed PMID: 23678595.

10: Cartwright AL, Wilby KJ, Corrigan S, Ensom MH. Pharmacogenetics of risperidone: a systematic review of the clinical effects of CYP2D6 polymorphisms. Ann Pharmacother. 2013 Mar;47(3):350-60. doi: 10.1345/aph.1R333. Epub 2013 Mar 5. Review. PubMed PMID: 23463739.

11: Manfredi G, Solfanelli A, Dimitri G, Cuomo I, Sani G, Kotzalidis GD, Girardi P. Risperidone-induced leukopenia: a case report and brief review of literature. Gen Hosp Psychiatry. 2013 Jan-Feb;35(1):102.e3-6. doi: 10.1016/j.genhosppsych.2012.03.009. Epub 2012 Apr 18. Review. PubMed PMID: 22520716.

12: Duhig MJ, Saha S, Scott JG. Efficacy of risperidone in children with disruptive behavioural disorders. J Paediatr Child Health. 2013 Jan;49(1):19-26. doi: 10.1111/j.1440-1754.2011.02200.x. Epub 2011 Nov 3. Review. PubMed PMID: 22050179.

13: Llerena A, Berecz R, Peñas-Lledó E, Süveges A, Fariñas H. Pharmacogenetics of clinical response to risperidone. Pharmacogenomics. 2013 Jan;14(2):177-94. doi: 10.2217/pgs.12.201. Review. PubMed PMID: 23327578.

14: Yang HN, Cheng YM. Peripheral edema associated with risperidone oral solution: a case report and a review of the literature. J Clin Psychopharmacol. 2012 Feb;32(1):128-30. doi: 10.1097/JCP.0b013e31823f8757. Review. PubMed PMID: 22217945.

15: Germann D, Kurylo N, Han F. Risperidone. Profiles Drug Subst Excip Relat Methodol. 2012;37:313-61. doi: 10.1016/B978-0-12-397220-0.00008-8. Epub 2012 Mar 19. Review. PubMed PMID: 22469322.

16: Bocharov AV, Kondakova VE, Tuleninov ES. [Efficasy and safety of the use of risperidone (rispoluxe) in demented patients with psychotic and behavioural disorders]. Zh Nevrol Psikhiatr Im S S Korsakova. 2012;112(6):25-31. Review. Russian. PubMed PMID: 22983233.

17: Glatstein M, Sulowski C, Waisburg C, Koren G, Garcia-Bournissen F. Severe extrapiramidal symptoms after nonintentional risperidone exposure in a child: case report and review of the literature. Am J Ther. 2011 Nov;18(6):e271-3. doi: 10.1097/MJT.0b013e3181debe49. Review. PubMed PMID: 20543664.

18: Seto K, Dumontet J, Ensom MH. Risperidone in schizophrenia: is there a role for therapeutic drug monitoring? Ther Drug Monit. 2011 Jun;33(3):275-83. doi: 10.1097/FTD.0b013e3182126d83. Review. PubMed PMID: 21436762.

19: Komossa K, Rummel-Kluge C, Schwarz S, Schmid F, Hunger H, Kissling W, Leucht S. Risperidone versus other atypical antipsychotics for schizophrenia. Cochrane Database Syst Rev. 2011 Jan 19;(1):CD006626. doi: 10.1002/14651858.CD006626.pub2. Review. PubMed PMID: 21249678; PubMed Central PMCID: PMC4167865.

20: Owenby RK, Brown LT, Brown JN. Use of risperidone as augmentation treatment for major depressive disorder. Ann Pharmacother. 2011 Jan;45(1):95-100. doi: 10.1345/aph.1P397. Epub 2010 Dec 28. Review. PubMed PMID: 21189367.