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CAS No.: 635323-95-4

F-15599 Catalog No. CSN24769

Synonyms: NLX-101;F-15,599

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist with Ki value of 3.4nM.

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实验方案

技术信息

生物活性

描述F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM. F15599 (0.06 or 0.12 mg/kg) significantly reduces l-DOPA-induced dyskinesia (LID), without affecting motor performance of rats. Rats treated with F15599 manifest less LID and mild 5-HT syndrome with the high dose of 30 μg/μL^[1]. Systemic administration of F15599 and F13714 exerted very potent (ID50 = 0.095 and 0.0059 mg/kg, respectively) anti-aggressive effects. Starting from the 0.25 mg/kg dose, F15599 induces clear signs of the so-called serotonin syndrome characterized by flat body posture, head-waving, lower lip retraction and hindlimb abduction, leading to increased behavioural inactivity scores and social disengagement^[2]. F15599 increased the discharge rate of pyramidal neurones in medial prefrontal cortex (mPFC) from 0.2 mg/kg i.v and reduced that of dorsal raphe 5-hydroxytryptaminergic neurones at doses >10-fold higher (minimal effective dose 8.2 mg/kg i.v.). F15599 did not alter low frequency oscillations (approximately 1 Hz) in mPFC. In microdialysis studies, F15599 increased dopamine output in mPFC (an effect dependent on the activation of postsynaptic 5-HT(1A) receptors) with an ED(50) of 30 mg/kg i.p., whereas it reduced hippocampal 5-HT release (an effect dependent exclusively on 5-HT(1A) autoreceptor activation) with an ED(50) of 240 mg/kg i.p. Likewise, application of F15599 by reverse dialysis in mPFC increased dopamine output in a concentration-dependent manner. All neurochemical responses to F15599 were prevented by administration of (+/-)WAY100635^[3].
参考文献

[1] Meadows SM, Chambers NE, Conti MM, et al. Characterizing the differential roles of striatal 5-HT1A auto- and hetero-receptors in the reduction of l-DOPA-induced dyskinesia. Exp Neurol. 2017;292:168-178
[2] de Boer SF, Newman-Tancredi A. Anti-aggressive effects of the selective high-efficacy 'biased' 5-HT₁A receptor agonists F15599 and F13714 in male WTG rats. Psychopharmacology (Berl). 2016;233(6):937-947
[3] Lladó-Pelfort L, Assié MB, Newman-Tancredi A, Artigas F, Celada P. Preferential in vivo action of F15599, a novel 5-HT(1A) receptor agonist, at postsynaptic 5-HT(1A) receptors. Br J Pharmacol. 2010;160(8):1929-1940

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5326 mL
- 12.6632 mL
- 25.3263 mL
- 5 mM
- 0.5065 mL
- 2.5326 mL
- 5.0653 mL
- 10 mM
- 0.2533 mL
- 1.2663 mL
- 2.5326 mL

技术信息

CAS号

635323-95-4

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21ClF2N4O

运输

蓝冰

分子量

394.85

别名

NLX-101;F-15,599

溶解度

DMSO	140.0 mg/mL (354.6 mM)
Water	insoluble

动物实验配方

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