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Palonosetron Hydrochloride

CAS No.
135729-62-3
Chemical Name:
Palonosetron Hydrochloride
Synonyms
PALONOSETRON HCL;Aloxi;Palonosetron HCI;Onicit;CS-292;RS 25259;RS-25259-197;PalnosetronHcl;a 5-HT3 antagonist;Palonosetron-d3 HCl
CBNumber:
CB0210849
Molecular Formula:
C19H25ClN2O
Molecular Weight:
332.87
MDL Number:
MFCD07370072
MOL File:
135729-62-3.mol
MSDS File:
SDS
Last updated:2024-11-20 15:18:15

Palonosetron Hydrochloride Properties

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)
NCI Dictionary of Cancer Terms Aloxi; palonosetron hydrochloride
FDA UNII 23310D4I19
NCI Drug Dictionary Aloxi

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H332-H302-H312
Precautionary statements  P264-P270-P301+P312-P330-P501-P280-P302+P352-P312-P322-P363-P501-P261-P271-P304+P340-P312
HS Code  29339900

Palonosetron Hydrochloride price More Price(39)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TCI Chemical P2051 Palonosetron Hydrochloride >98.0%(HPLC)(T) 135729-62-3 200mg $215 2024-03-01 Buy
TCI Chemical P2051 Palonosetron Hydrochloride >98.0%(HPLC)(T) 135729-62-3 1g $741 2024-03-01 Buy
Cayman Chemical 16752 Palonosetron (hydrochloride) ≥98% 135729-62-3 5mg $73 2024-03-01 Buy
Cayman Chemical 16752 Palonosetron (hydrochloride) ≥98% 135729-62-3 10mg $131 2024-03-01 Buy
Cayman Chemical 16752 Palonosetron (hydrochloride) ≥98% 135729-62-3 50mg $359 2024-03-01 Buy
Product number Packaging Price Buy
P2051 200mg $215 Buy
P2051 1g $741 Buy
16752 5mg $73 Buy
16752 10mg $131 Buy
16752 50mg $359 Buy

Palonosetron Hydrochloride Chemical Properties,Uses,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 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]

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 HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting

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

Global( 508)Suppliers
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View Lastest Price from Palonosetron Hydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Palonosetron Hydrochloride pictures 2024-12-13 Palonosetron Hydrochloride
135729-62-3
US $0.00 / KG 10g 99%min 10kg WUHAN FORTUNA CHEMICAL CO., LTD
Palonosetron Hydrochloride pictures 2024-11-20 Palonosetron Hydrochloride
135729-62-3
US $1.00 / KG 1KG 99% 10 mt Hebei Weibang Biotechnology Co., Ltd
Palonosetron hydrochloride pictures 2024-11-19 Palonosetron hydrochloride
135729-62-3
US $47.00-86.00 / mg 99.92% 10g TargetMol Chemicals Inc.

Palonosetron Hydrochloride Spectrum

PALONOSETRON HYDROCHLORIDE (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one Hydrochloride Onicit RS-25259-197 (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one monohydrochloride (S,S)-Palonosetron Hydrochloride (S,S)-Palonosetron HCl (3aS)-2-[(S)-1-Azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1-oxo-1H-benz[de]isoquinoline hydrochloride Palonosetron Hydrochloride API 1H-Benz[de]isoquinolin-1-one, 2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-, hydrochloride (1:1), (3aS)- RS 25259 (S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one hydrochloride Palonosetron hydrochloride, >=99% Palonosetron hydrochloride, 99.5%, a 5-HT3 antagonist CS-292 Palonosetronhydrochloride hydrochloride Palonosetron-d3 HCl PalonosetronHydrochloride> (S)-8-((((S)-quinuclidin-3-yl)amino)methyl)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Palonosetron Hydrochloride USP/EP/BP a 5-HT3 antagonist PalnosetronHcl Palonosetron HCl (RS25233-197 (5S)-3-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3-azatricyclo[7.3.1.?,13]trideca-1(13),9,11-trien-2-one hydrochloride Palonosetron Hydrochloride (1492200) Methylisothiazolinone free base (S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5 PALONOSETRON HCL Aloxi Palonosetron HCI RS 25259 197|||Palonosetron HCl|||RS 25259 135729-62-3 C19H24N2OHCl C19H25ClN2O C19H24N2OHC Selective 5-HT3 Receptor Antagonist Chiral Reagents Heterocycles Intermediates & Fine Chemicals Pharmaceuticals API 135729-62-3