Palonosetron Hydrochloride

Bezeichnung:Palonosetron Hydrochloride

CAS-Nr135729-62-3

Englisch Name:Palonosetron Hydrochloride

CBNumberCB0210849

SummenformelC19H25ClN2O

Molgewicht332.87

MOL-Datei135729-62-3.mol

Palonosetron Hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	>290°C
alpha	D25 -94.1° (c = 0.4 in water)
storage temp.	Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	Methanol (Slightly, Heated), Water (Slightly)
Aggregatzustand	Solid
Farbe	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 Datenbank	135729-62-3(CAS DataBase Reference)

Sicherheit

HS Code

29339900

Gefahreninformationscode (GHS)

Bildanzeige (GHS)
Alarmwort

Warnung
Gefahrenhinweise

H302：Gesundheitsschädlich bei Verschlucken.

H312：Gesundheitsschädlich bei Hautkontakt.

H332：Gesundheitsschädlich bei Einatmen.
Sicherheit

P261：Einatmen von Staub vermeiden.

P264：Nach Gebrauch gründlich waschen.

P264：Nach Gebrauch gründlich waschen.

P270：Bei Gebrauch nicht essen, trinken oder rauchen.

P271：Nur im Freien oder in gut belüfteten Räumen verwenden.

P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

P301+P312：BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

P302+P352：BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.

P304+P340：BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen.

P312：Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

P322：Gezielte Maßnahmen

P330：Mund ausspülen.

P363：Kontaminierte Kleidung vor erneutem Tragen waschen.

P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Palonosetron Hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
White Solid
Originator
Syntex (Roche Bioscience) (US)
Verwenden
(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.
Verwenden
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]
Verwenden
specifically inhibits cells of the adrenal cortex and their production of hormones for adrenocortical tumor therapy, causes CNS damage, but no bone marrow depression.
Verwenden
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.
Trademarks
Aloxi (Helsinn).
Lager
Store at -20°C

Palonosetron Hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

135729-62-3, Palonosetron Hydrochloride Verwandte Suche:

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