Palonosetron Hydrochloride
Nausea and vomiting drug Adverse effects References- Product Name
- Palonosetron Hydrochloride
- CAS No.
- 135729-62-3
- Chemical Name
- Palonosetron Hydrochloride
- Synonyms
- PALONOSETRON HCL;Aloxi;Palonosetron HCI;CS-292;Onicit;RS 25259;RS-25259-197;PalnosetronHcl;a 5-HT3 antagonist;Palonosetron-d3 HCl
- CBNumber
- CB0210849
- Molecular Formula
- C19H25ClN2O
- Formula Weight
- 332.87
- MOL File
- 135729-62-3.mol
Palonosetron Hydrochloride Property
- Melting point:
- >290°C
- alpha
- D25 -94.1° (c = 0.4 in water)
- storage temp.
- Inert atmosphere,Store in freezer, under -20°C
- solubility
- Methanol (Slightly, Heated), Water (Slightly)
- form
- Solid
- color
- White to Off-White
- Merck
- 14,6997
- InChI
- InChI=1/C19H24N2O.ClH/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;1H/t15-,17-;/s3
- InChIKey
- OLDRWYVIKMSFFB-HYCRUXCXNA-N
- SMILES
- N1(C[C@@]2([H])CCCC3=CC=CC(=C32)C1=O)[C@H]1[C@]2([H])CCN(CC2)C1.Cl |&1:2,15,16,r|
- CAS DataBase Reference
- 135729-62-3(CAS DataBase Reference)
Safety
- HS Code
- 29339900
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H312Harmful in contact with skin
H332Harmful if inhaled
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P322Specific measures (see …on this label).
P330Rinse mouth.
P363Wash contaminated clothing before reuse.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- P2051
- Product name
- Palonosetron Hydrochloride
- Purity
- >98.0%(HPLC)(T)
- Packaging
- 200mg
- Price
- $215
- Updated
- 2024/03/01
- Product number
- P2051
- Product name
- Palonosetron Hydrochloride
- Purity
- >98.0%(HPLC)(T)
- Packaging
- 1g
- Price
- $741
- Updated
- 2024/03/01
- Product number
- 16752
- Product name
- Palonosetron (hydrochloride)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 16752
- Product name
- Palonosetron (hydrochloride)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $131
- Updated
- 2024/03/01
- Product number
- 16752
- Product name
- Palonosetron (hydrochloride)
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $359
- Updated
- 2024/03/01
Palonosetron Hydrochloride Chemical Properties,Usage,Production
Nausea and vomiting drug
Palonosetron hydrochloride is a drug to inhibit nausea and vomiting, which is a new type highly selective, high-affinity 5-HT3 receptor antagonist that can block the vomiting reflex center peripheral neurons presynaptic 5-HT. Receptor excitement directly affects the central nervous system in 5-HT. Impulse receptor excitement generated by the role of vagal afferent nerve after area, blocking the vagus nerve endings in the gut, preventing signals to 5-HT. Receptor trigger zone can reduce the incidence of nausea and vomiting. Central clinically for the treatment of acute severe emetogenic chemotherapy induced delayed nausea and vomiting. Because of its high curative effect, little side effect, long half-life (about 40 h), small dosage, and so on, it has attracted much attention.
With 1,2,3,4-tetrahydro-1-naphthoic acid as the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
Clinical studies showed that palonosetron can be used safely with corticosteroids, analgesics, antiemetics, antispasmodics and anticholinergic drugsas the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
Murine tumor model studies indicate that palonosetron does not inhibit the five kinds of chemotherapy drugs studied (cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin C) anti-cancer activity.
Adverse effects
The most common adverse effects are headache, which occurs in 4–11% of patients, and constipation in up to 6% of patients. In less than 1% of patients, other gastrointestinal disorders occur, as well as sleeplessness, first-and second-degree atrioventricular block, muscle pain and shortness of breath. Palonosetron is similarly well tolerated as other setrons, and slightly less than placebo.
References
https://en.wikipedia.org/wiki/Palonosetron
Description
Palonosetron is a novel 5-HT3 receptor antagonist launched as an injectable agent for the prevention of acute and delayed nausea and vomiting associated with cancer chemotherapy. It has a much longer half-life (～ 40 h) than the other currently available 5-HT3 antagonists, which provides efficacy advantages in the prevention of delayed nausea and vomiting that typically occurs after 24 h and up to six days post chemotherapy administration. Palonosetron was developed as a conformationally restricted analog of the previously known 5HT3 antagonists tropisetron and granisetron. It is synthesized in four steps starting with the condensation of 1,8- naphthalic anhydride and (S)-3-aminoquinuclidine to produce the corresponding imide. The subsequent steps include catalytic hydrogenation of one of the aromatic rings of the imide intermediate, selective reduction of one of the carbonyls to a hydroxyl group, dehydration to an olefin and catalytic hydrogenation. The recommended dosage of palonosteron is 0.25 mg, administered as a single intravenous dose approximately 30 min before the start of chemotherapy. Palonosetron exhibits dose-proportional pharmacokinetics and it is moderately bound to plasma proteins (62%). Fifty percent of the dose is metabolized in the liver, and 40% is excreted unchanged in the urine. In comparative clinical studies with two other 5- HT3 receptor antagonists, palonosetron is shown to be as effective as dolasetron and more effective than ondansetron in controlling acute nausea and vomiting and superior to both in the control of delayed nausea and vomiting. Efficacy of palonosetron has been demonstrated in patients receiving initial and repeat courses of both moderately and highly emetogenic chemotherapy, including cisplatin, cyclophosphamide and dacarbazine. At 0.25 and 0.75 mg doses, palonosetron is well tolerated and the most occurring adverse events are headache, diarrhea, fatigue, abdominal pain and insomnia.
Chemical Properties
White Solid
Originator
Syntex (Roche Bioscience) (US)
Uses
(S,S)-Palonosetron Hydrochloride is a serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). Antiemetic.
Uses
Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting
Uses
specifically inhibits cells of the adrenal cortex and their production of hormones for adrenocortical tumor therapy, causes CNS damage, but no bone marrow depression.
Uses
Palonosetron is a potent, selective antagonist of the serotonin (5-HT) receptor 5-HT3 (pKi = 10.4 in rat cortex) that minimally effects a wide range of other neuronal receptors. It is orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs, like cisplatin , but not by apomorphine , which acts by dopamine receptor antagonism. Palonosetron is remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life. It is effective in managing chemotherapy-induced nausea and vomiting.[Cayman Chemical]
Definition
ChEBI: A hydrochloride obtained by combining palonosetron with one molar equivalent of hydrogen chloride; an antiemetic used in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.
brand name
Aloxi (Helsinn).
storage
Store at -20°C
Palonosetron Hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Palonosetron Hydrochloride manufacturers
- Product
- Palonosetron Hydrochloride 135729-62-3
- Price
- US $428.70/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 1t
- Release date
- 2023-07-21
- Product
- Palonosetron hydrochloride 135729-62-3
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98% HPLC
- Supply Ability
- 100kg
- Release date
- 2023-08-14
- Product
- Palonosetron Hydrochloride 135729-62-3
- Price
- US $0.00/KG
- Min. Order
- 10g
- Purity
- 99%min
- Supply Ability
- 10kg
- Release date
- 2021-11-02