Azasetron (hydrochloride)

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mM*1mL (in Water)
ArtNr HY-B0068-10mM
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
Y-25130 hydrochloride, Y25130 hydrochloride, Y 25130 hydrochloride
CAS No.
123040-16-4
Purity
>98%
MW
3862729
Formula
C17H21Cl2N3O3
Solubility
H2O:>= 3.9 mg/mL
Biological Description
Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.
Target: 5-HT3 Receptor
Azasetron Hydrochloride is a 5-HT3 receptor antagonist which is used as an anti-emetic.
Azasetron inhibited the specific binding of [3H]quipazine to 5-HT3 receptors at the synaptic membranes of the rat cerebral cortex with a Ki value of 2.9 nM. Azasetron showed low affinity for histamine H1 receptors (IC50 = 4.4 microM) but it could not reveal any affinities for the other receptors (5-HT1A, 5-HT2, dopamine D1, dopamine D2, alpha 1-adrenoceptor, alpha 2-adrenoceptor, muscarine and benzodiazepine) even at a 10 microM concentration [1]. Azasetron (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. Azasetron is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone [2].
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Menge: 10mM*1mL (in Water)
Lieferbar: In stock
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Rabatt: -10,0%
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