Palonosetron

• CAT Number: I001384
• CAS Number: 135729-61-2
• Molecular Formula: C19H24N2O
• Molecular Weight: 296.41
• Purity: 90%
• Target: HTR3A TACR1
• Target Protein: P25103
• Solubility: 10 mM in DMSO
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IUPAC Name: (3aS)-2-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3a,4,5,6-tetrahydro-3H-benzo[de]isoquinolin-1-one
• InChI: InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1
• InChIKey: CPZBLNMUGSZIPR-NVXWUHKLSA-N
• SMILES: C1C[C@@H]2CN(C(=O)C3=CC=CC(=C23)C1)[C@@H]4CN5CCC4CC5

Palonosetron（Cat No.:I001384）is a long-acting serotonin (5-HT3) receptor antagonist used to prevent nausea and vomiting caused by chemotherapy, radiation therapy, and surgery. It works by blocking the action of serotonin, a key neurotransmitter involved in triggering the vomiting reflex, particularly in the gastrointestinal tract. Palonosetron has a longer half-life compared to other 5-HT3 antagonists, offering extended protection against both acute and delayed chemotherapy-induced nausea and vomiting. Its high receptor affinity and improved duration of action make it a preferred choice for patients undergoing highly emetogenic cancer treatments.

Reference

[1]. Clark, Robin D.; Miller, Aaron B.; Berger, Jacob; Repke, David B.; Weinhardt, Klaus K.; Kowalczyk, Bruce A.; Eglen, Richard M.; Bonhaus, Douglas W.; Lee, Chi Ho; et al.2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists.J. Med. Chem., 1993, 36 (18), pp 2645-2657

[2]. Celio L, Agustoni F, Testa I, Dotti K, De Braud F.Palonosetron: an evidence-based choice in prevention of nausea and vomiting induced by moderately emetogenic chemotherapy.Tumori. 2012 May;98(3):279-86.

[3]. Blazer M, Phillips G, Reardon J, Efries D, Smith Y, Weatherby L, Juergens K, Rose J, Griffith N, Bekaii-Saab T.Antiemetic control with palonosetron in patients with gastrointestinal cancer receiving a fluoropyrimidine-based regimen in addition to either irinotecan or oxaliplatin: a retrospective study.Oncology. 2012;83(3):135-40. Epub 2012 Jul 18.

[4]. Dogan U, Yavas G, Tekinalp M, Yavas C, Ata OY, Ozdemir K.Evaluation of the acute effect of palonosetron on transmural dispersion of myocardial repolarization.Eur Rev Med Pharmacol Sci. 2012 Apr;16(4):462-8.

[5]. Jin Y, Sun W, Gu D, Yang J, Xu Z, Chen J.Comparative efficacy and safety of palonosetron with the first 5-HT3 receptor antagonists for the chemotherapy-induced nausea and vomiting: a meta-analysis.Eur J Cancer Care (Engl). 2012 Apr 22.