For research use only. Not for therapeutic Use.
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
| Catalog Number | M097923 |
| CAS Number | 143257-98-1 |
| Synonyms | Lerisetron |
| Molecular Formula | C18H20N4 |
| Purity | ≥95% |
| Target | Neuronal Signaling |
| Storage | Store at RT |
| IUPAC Name | 1-benzyl-2-piperazin-1-ylbenzimidazole |
| InChI | InChI=1S/C18H20N4/c1-2-6-15(7-3-1)14-22-17-9-5-4-8-16(17)20-18(22)21-12-10-19-11-13-21/h1-9,19H,10-14H2 |
| InChIKey | PWWDCRQZITYKDV-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1)C2=NC3=CC=CC=C3N2CC4=CC=CC=C4 |
| Reference | </br>1:Pharmacokinetic-pharmacodynamic modeling of the hydroxy lerisetron metabolite L6-OH in rats: an integrated parent-metabolite model. Ortega F, Quintana A, Suárez E, Lukas JC, Jauregizar N, de la Fuente L, Lucero ML, Gonzalo A, Orjales A, Calvo R.Pharm Res. 2005 Nov;22(11):1769-82. Epub 2005 Sep 20. PMID: 16158214 </br>2:Lerisetron. FAES. Huckle R.Curr Opin Investig Drugs. 2003 Jul;4(7):874-7. Review. PMID: 14619411 </br>3:Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model. Jauregizar N, Quintana A, Suarez E, Raczka E, de la Fuente L, Calvo R.Gerontology. 2003 Jul-Aug;49(4):205-14. PMID: 12792155 </br>4:Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers. Cooper M, Sologuren A, Valiente R, Smith J.Arzneimittelforschung. 2002;52(9):689-94. PMID: 12404884 </br>5:Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. Jauregizar N, Calvo R, Suarez E, Quintana A, Raczka E, Lukas JC.J Pharm Sci. 2002 Jan;91(1):41-52. PMID: 11782896 </br>6:5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions. Parihar HS, Suryanarayanan A, Ma C, Joshi P, Venkataraman P, Schulte MK, Kirschbaum KS.Bioorg Med Chem Lett. 2001 Aug 20;11(16):2133-6. PMID: 11514154 </br>7:Altered disposition and effect of lerisetron in rats with elevated alpha 1-acid glycoprotein levels. Jauregizar N, Calvo R, Suarez E, Quintana A, Raczka E, Lukas JC.Pharm Res. 2001 Jun;18(6):838-45. PMID: 11474789 </br>8:Lerisetron. F 0930, F 0930RS. [No authors listed]Drugs R D. 1999 Oct;2(4):245-6. No abstract available. PMID: 10659400 </br>9:Antiemetic effects of Lerisetron in radiation-induced emesis in the dog. Gomez-de-Segura IA, Grande AG, De Miguel E.Acta Oncol. 1998;37(7-8):759-63. PMID: 10050999 </br>10:Serum protein binding of lerisetron, a novel specific 5HT3 antagonist, in patients with cancer. Calvo R, Jiménez RM, Trocóniz IF, Suárez E, Gonzalo A, Lucero ML, Raczka E, Orjales A.Cancer Chemother Pharmacol. 1998;42(5):418-22. PMID: 9771958 |
