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LY310762

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Chemical Structure| 192927-92-7 同义名 : LY310762 HCl
CAS号 : 192927-92-7
货号 : A161442
分子式 : C24H28ClFN2O2
纯度 : 99%+
分子量 : 430.943
MDL号 : MFCD07772272
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(37.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • 5-HT1

    5-HT1D, Ki:249 nM
描述 LY310762 is a 5-HT1D receptor antagonist (Ki = 249 nM). with a weaker affinity for 5-HT1B receptor. LY310762, is more effective at potentiating [3H]5-HT release from guinea pig cortical slices (EC50 = 31 ± 6 nM). LY310762 potentiated the potassium-induced [3H]5-HT outflow from guinea pig cortical slices with EC50 values in the range 30 - 140 nM. In vivo, systemic administration of LY310762 (10 mg/kg i.p.) also produced a further significant enhancement in the 5-HT[3]. LY310762 (10 µM) blocks the decreased EPSC amplitude induced by sumatriptan[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.60mL

2.32mL

1.16mL

23.20mL

4.64mL

2.32mL
参考文献

[1]Choi IS, Cho JH, et al. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012 Sep;167(2):356-67.

[2]Pullar IA, Boot JR, et al. The role of the 5-HT1D receptor as a presynaptic autoreceptor in the guinea pig. Eur J Pharmacol. 2004 Jun 16;493(1-3):85-93.

[3]Pullar IA, Boot JR, Broadmore RJ, et al. The role of the 5-HT1D receptor as a presynaptic autoreceptor in the guinea pig. Eur J Pharmacol. 2004;493(1-3):85-93.

[4]Choi IS, Cho JH, An CH, et al. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012;167(2):356-367.