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).
Orally active, potent and selective 5-HT3 receptor antagonist with in vivo antiemetic efficacy.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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European journal of pharmacology, 196(3), 299-305 (1991-04-24)
Y-25130( (+/-)N-(1-azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro - 2H-1,4-benzoxazine-8-carboxamide hydrochloride) is a potent and selective 5-HT3 receptor antagonist free of dopamine receptor blocking activity. This compound was effective against emesis induced in animals by cytotoxic drugs or by total body X-radiation. When given prophylactically, the
Japanese journal of pharmacology, 73(4), 357-360 (1997-04-01)
The binding affinity of azasetron hydrochloride (azasetron) for the 5-hydroxytryptamine3 (5-HT3) receptor in a tissue preparation of rat small intestine was investigated by using [3H]granisetron as a radioligand. Scatchard analysis of specific [3H]granisetron binding revealed a single population of saturable
Japanese journal of pharmacology, 80(1), 25-32 (1999-08-14)
5-Hydroxytryptamine3 (5-HT3)-receptor blocking activities of KB-R6933 (6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)-benzimidazole dimaleate) were assessed in vivo and in vitro. Intravenous administration of KB-R6933, granisetron, ondansetron and azasetron inhibited 5-HT-induced bradycardia (von Bezold-Jarisch reflex) in anesthetized rats, with ED50 values of 0.071, 0.71, 4.0 and
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