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  • LY 344864
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LY 344864

A 5-HT1F receptor antagonist

原价
¥962-4100
价格
770-3280
LY 344864的二维码

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  • 货号: ajci18320
  • CAS: 186544-26-3
  • 别名: LY344864;LY-344864
  • 分子式: C21H22FN3O
  • 分子量: 351.42
  • 纯度: >98%
  • 溶解度: DMSO : ≥ 350 mg/mL (995.96 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

IC50 Value: 6 nM(Ki) LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. It possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1]. in vitro: he 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs [2]. in vivo: After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels declined with time whereas brain cortex levels remained relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibited dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Sumatriptan, zolmitriptan, rizatriptan, and naratriptan all contracted the rabbit saphenous vein from baseline tone, whereas LY344864 in concentrations up to 10(-4) M did not contract the rabbit saphenous vein. Furthermore, vascular contractions to sumatriptan were markedly augmented in the presence of prostaglandin F(2alpha) (PGF(2alpha)). However, even in the presence of PGF(2alpha) (3 x 10(-7) M), LY344864 did not contract the rabbit saphenous vein in concentrations well in excess of its 5-HT(1F) receptor affinity (pK(i) = 8.2) [3]. Clinical trial: N/A

Protocol

Animal experiment:

Rats[2]Male albino Wistar rats are divided into different groups. Rats in the experimental LY344864 and sham groups receive LY 344864 (1 or 2 μg/5 μL; intracerebroventricular [i.c.v.]), vehicle (5 μl/rat i.c.v.), or saline (5 μl/rat i.c.v.) during the acquisition phase[2]

参考文献:

[1]. Phebus LA, et al. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26.
[2]. Shahidi S, et al. Intracerebroventricular microinjection of the 5-HT1F receptor agonist LY 344864 inhibits methamphetamine conditioned place preference reinstatement in rats. Pharmacol Biochem Behav. 2018 Aug 2.

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