Palonosetron5-HT3 antagonist CAS# 135729-61-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 135729-61-2 | SDF | Download SDF |
| PubChem ID | 148211 | Appearance | Powder |
| Formula | C19H24N2O | M.Wt | 296.42 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO | ||
| Chemical Name | (3aR)-2-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3a,4,5,6-tetrahydro-3H-benzo[de]isoquinolin-1-one | ||
| SMILES | C1CC2CN(C(=O)C3=C2C(=CC=C3)C1)C4CN5CCC4CC5 | ||
| Standard InChIKey | CPZBLNMUGSZIPR-DOTOQJQBSA-N | ||
| Standard 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+/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Palonosetron Dilution Calculator
Palonosetron Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.3736 mL | 16.868 mL | 33.7359 mL | 67.4718 mL | 84.3398 mL |
| 5 mM | 0.6747 mL | 3.3736 mL | 6.7472 mL | 13.4944 mL | 16.868 mL |
| 10 mM | 0.3374 mL | 1.6868 mL | 3.3736 mL | 6.7472 mL | 8.434 mL |
| 50 mM | 0.0675 mL | 0.3374 mL | 0.6747 mL | 1.3494 mL | 1.6868 mL |
| 100 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.6747 mL | 0.8434 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Palonosetron (trade name Aloxi) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).Palonosetron (trade name Aloxi) is useful for antiemetic and antinauseant
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Efficacy of NEPA (netupitant/palonosetron) across multiple cycles of chemotherapy in breast cancer patients: A subanalysis from two phase III trials.[Pubmed:28285236]
Breast. 2017 Jun;33:76-82.
OBJECTIVES: Breast cancer (BC) patients represent a high-risk population for experiencing chemotherapy-induced nausea and vomiting (CINV), since they frequently receive highly emetogenic anthracycline-cyclophosphamide-based (AC) chemotherapy, and are often female and young, two predisposing risk factors for CINV. Guidelines recommend the combination of a neurokinin-1 receptor antagonist (NK1RA), 5-hydroxytryptamine-3 RA (5-HT3RA), and dexamethasone (DEX) for CINV prophylaxis in AC-treated patients. This post-hoc analysis evaluated the efficacy of NEPA, a fixed combination of netupitant (NETU [NK1RA]) and Palonosetron (PALO [5-HT3RA]) in BC patients from two phase III studies. METHODS: Overall, 1460 BC patients received AC (Study 1) or non-AC (Study 2) therapy over 6060 cycles. Randomized patients received DEX with either NEPA or oral PALO (Study 1), or NEPA or aprepitant+oral PALO (Study 2) before chemotherapy. RESULTS: In AC-receiving patients, overall complete response (CR) rates with NEPA+DEX were statistically significantly higher than oral PALO+DEX rates (cycles 1-4: 73.9% vs 65.9%, 80.0% vs 66.0%, 83.6% vs 69.9%, 83.6% vs 74.4%, respectively). Overall, no significant nausea (NSN) rates were also superior with NEPA+DEX vs oral PALO+DEX (respectively, 74.2%-79.9% vs 68.5%-74.9%). A greater proportion of NEPA+DEX patients experienced "no-impact-on-daily-life" due to CINV (78.4% vs 71.4%) in cycle 1. In non-AC-receiving patients, prophylaxis with NEPA+DEX resulted in high CR and NSN rates across 1-4 chemotherapy cycles; no formal comparison with the control arm was performed. CONCLUSION: NEPA+DEX administered as a single dose is an effective option for preventing CINV in BC patients receiving AC and non-AC, across multiple chemotherapy cycles. CLINICAL TRIALS REGISTRATION NUMBERS: Study 1: NCT01339260, Study 2:NCT01376297.
Comparison of Ramosetron with Palonosetron for Prevention of Postoperative Nausea and Vomiting in Patients Receiving Opioid-Based Intravenous Patient-Controlled Analgesia after Gynecological Laparoscopy.[Pubmed:28357406]
Biomed Res Int. 2017;2017:9341738.
We aimed to compare the effects of ramosetron and Palonosetron in the prevention of postoperative nausea and vomiting (PONV) in patients that received opioid-based intravenous patient-controlled analgesia (IV-PCA) after gynecological laparoscopy. We reviewed the electronic medical records of 755 adults. Patients were classified into two groups, ramosetron (group R, n = 589) versus Palonosetron (group P, n = 166). Based on their confounding factors, 152 subjects in each group were selected after the implementation of propensity score matching. The overall incidence of PONV at postoperative day (POD) 0 was lower in group R compared to group P (26.9% versus 36.8%; P = 0.043). The severity of nausea was lower in group R than in group P on postoperative day (POD) 0 (P = 0.012). Also, the complete responder proportion of patients was significantly higher in group R compared to that in group P on POD 0 (P = 0.043). In conclusion, ramosetron showed a greater efficacy in the prevention of postoperative nausea at POD 0 compared to Palonosetron in patients after gynecological laparoscopy.
Intravenous palonosetron compared with a combination of ramosetron and dexamethasone in preventing post operative nausea and vomiting in patients undergoing gynaecological surgeries under spinal anaesthesia, a randomised study.[Pubmed:28250483]
Indian J Anaesth. 2017 Feb;61(2):144-149.
BACKGROUND AND AIMS: Post-operative nausea and vomiting (PONV) is one of the most common complications in patients undergoing gynaecological surgeries under spinal anaesthesia (SA). Palonosetron has the unique property of controlling 'delayed chemotherapy-induced nausea and vomiting' when compared to older serotonin antagonists. This study compared the effectiveness of Palonosetron with a combination of ramosetron and dexamethasone in preventing PONV. METHODS: Sixty patients undergoing gynaecological surgeries under SA were randomly allocated into two groups of thirty each, to receive either a combination of 0.3 mg of ramosetron and 8 mg of dexamethasone intravenously (IV) (Group RD) or 0.075 mg of Palonosetron IV (Group P). The incidence of PONV, number of complete responders (no nausea, vomiting or use of rescue anti-emetics) and severity of nausea were evaluated during intra- and post-operative period. RESULTS: The incidence of complete responders during intraoperative period was 80.0% in Group RD and 76.7% in Group P (P = 0.074) whereas postoperatively at 0-2 h and 2-6 h, it was 73.3% and 83.3% in Group RD respectively as compared to 46.6% and 56.6% in Group P respectively (P = 0.016 and P = 0.024). The incidence of PONV during 24 h of post-operative period was 30.00% in Group RD as compared to 60.00% in Group P (P = 0.0195). Nausea severity score and use of rescue anti-emetics did not vary between the groups. CONCLUSION: Combination of ramosetron and dexamethasone is more effective than Palonosetron alone in preventing PONV in patients undergoing gynaecological surgeries under SA.
Effectiveness of antiemetic triplet therapy with aprepitant, palonosetron, and dexamethasone for gynecologic cancer patients receiving carboplatin and paclitaxel: a prospective single-arm study.[Pubmed:28160077]
Support Care Cancer. 2017 Jun;25(6):1941-1945.
PURPOSE: There is no positive evidence for the efficacy of antiemetic triplet therapy with aprepitant (APR), Palonosetron (PALO), and dexamethasone (DEX) for moderate emetogenic chemotherapy, especially for gynecologic malignancies. Thus, the present study evaluated the efficacy of this triplet therapy in patients receiving carboplatin and paclitaxel (CP) for gynecologic malignancy. METHODS: Seventy patients with gynecologic cancer receiving CP were enrolled into a prospective single-arm study with APR (125 mg on day 1, 80 mg on days 2-3), PALO (0.75 mg), and DEX (20 mg) before initiating chemotherapy. The primary endpoint was delayed complete response (CR) rate, i.e., no vomiting and no rescue, at 24-120 h after chemotherapy administration. RESULTS: Seventy patients were enrolled. The delayed CR rate was 97.1% (68/70). No serious adverse events were observed. Younger patient age (
