RG-12915

Names

[ Name ]:
RG-12915

[Synonym ]:
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

Biological Activity

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
462.6±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₂₅ClN₂O₂

[ Molecular Weight ]:
360.878

[ Flash Point ]:
233.6±28.7 °C

[ Exact Mass ]:
360.160461

[ LogP ]:
4.03

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.631

[ Storage condition ]:
2-8℃

Related Compounds

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