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  • RG-12915
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RG-12915

RG-12915是一种选择性的5-HT3拮抗剂,IC50值为0.16nM。

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¥10912-64537
价格
8730-51630
RG-12915的二维码

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  • 货号: ajce52558
  • CAS: 136174-04-4
  • 别名:
  • 分子式: C20H25ClN2O2
  • 分子量: 360.88
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.


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.


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].


[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.

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