AZASETRON HYDROCHLORIDE

AZASETRON HYDROCHLORIDE

Stock Code: 3576390
Manufacturer Part No: SML2491-25MG
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Biochem/physiol Actions


Azasetron (Y-25130) is an orally active, potent and selective 5-HT3 receptor antagonist (binding Ki = 0.33 nM against [3H]granisetron/rat small intestine, 2.9 nM against [3H]quipazine/rat cortex; little or no affinity toward H1,d5-HT1A/2, Dopamine D1/2, α1/α2 adrenoceptor, muscarinic receptors) with in vivo antiemetic efficacy (0.1-0.3 mg/kg i.v. & 0.1-1 mg/kg p.o.; dogs, ferrets). Y-25130 inhibits 5-HT-induced bradycardia in anesthetized rats (ED50 = 820 ng/kg i.v.), while concurrent intrahippocampal infusion (1.0 µg/side) prevents memory function impairment caused by muscarinic acetylcholine receptor antagonist scopolamine (3.2 µg/side), but not NMDA receptor antagonist CPP (32 ng/side).

Colourwhite to beige
InChI keyDBMKBKPJYAHLQP-UHFFFAOYSA-N
InChI1S/C17H20ClN3O3.ClH/c1-20-14-7-11(18)6-12(16(14)24-9-15(20)22)17(23)19-13-8-21-4-2-10(13)3-5-21;/h6-7,10,13H,2-5,8-9H2,1H3,(H,19,23);1H
ManufacturerSIGMA-ALDRICH
SolubilityH2O: 2 mg/mL, clear
Formpowder
Assay≥98% (HPLC)

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