Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: N-(1-azabicyclo(2.2.2)octan-3-yl)-2-chloro-5a,6,7,8,9,9a-hexahydrodibenzofuran-4-carboxamide
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Purity: 98.0%
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136174-04-4

136174-04-4 structure

Name	RG-12915
Synonyms	533O919MKO 4-Dibenzofurancarboxamide, N-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2-chloro-5a,6,7,8,9,9a-hexahydro-, (5aS,9aS)- (5aS,9aS)-N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-2-chloro-5a,6,7,8,9,9a-hexahydrodibenzo[b,d]furan-4-carboxamide

Description	RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Cancer
Target	IC50: 0.16 nM (5-HT3)[1]
In Vitro	RG 12915 is a potent and selective displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites (IC50 value = 0.16 nM), whereas failing to displace binding of ligands for the alpha-1, alpha-2 and beta adrenergic, 5-HT1 or 5-HT2 or cholinergic-muscarinic sites with IC50 values less than 1 μM.
In Vivo	RG 12915 has a lower ED50 value (0.004 mg/kg) for attenuating cisplatin-induced emetic episodes in the ferret. RG 12915 (1 mg/kg, p.o.) is highly protective against cisplatin-induced emesis in the dog. RG 12915 has no significant gastroprokinetic activity in the same species[1].
References	[1]. Fitzpatrick LR, et al. RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in the ferret and dog. J Pharmacol Exp Ther. 1990 Aug;254(2):450-5.