H672 Palonosetron hydrochloride - AK Scientific
 
 
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  Catalog ID # H672
Palonosetron hydrochloride
, 98%
 



IDENTITY
CAS Registry #:[135729-62-3]
MDL Number:MFCD07370072
MF:C19H24N2O.HCl
MW:332.8676
SPECIFICATIONS & PROPERTIES
Purity:98%
Physical Form:White crystalline powder
Melting Point:279-311°C
Optical Rotation:-94.1° (c=0.4 in water)
Shipping:Normal Temperature

BIOLOGICAL INFO
Application(s):5-HT3 antagonist
Form:HCl salt

REVIEW

 Palonosetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT3 receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron's potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy.

REFERENCES
[1]De Leon A: Palonosetron (Aloxi): a second-generation 5-HT receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent). 2006 Oct;19(4):413-6.
[2] Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31.
[3] Rubenstein EB: Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9.
[4] Yang LP, Scott LJ: Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000.

Risk Description(s)
R36/37/38:Irritating to eyes, respiratory system and skin

Safety Description(s)
S24/25:Avoid contact with skin and eyes.


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RELATED PRODUCTS
71897Palonosetron
H672Palonosetron hydrochloride

CATEGORIES

 APIs and Bioactives > Serotonin Antagonists

USEFUL LINKS

  PubChem