الصفحة الرئيسية>>Signaling Pathways>> Neuroscience>> 5-HT Receptor>>Befiradol hydrochloride (NLX-112 (hydrochloride))

Befiradol hydrochloride (NLX-112 (hydrochloride))

رقم الكتالوجGC34304

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Befiradol hydrochloride (NLX-112 (hydrochloride)) التركيب الكيميائي

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
556٫00
متوفر
5mg
506٫00
متوفر
10mg
782٫00
متوفر
25mg
1609٫00
متوفر
50mg
2528٫00
متوفر
100mg
3631٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Befiradol hydrochloride (NLX-112 (hydrochloride))

Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT1A receptor agonist.

Befiradol (F13640; NLX-112) reduces the activity of dorsal raphe serotonergic neurons at 0.2-18.2 μg/kg, i.v. (cumulative doses; ED50=0.69 μg/kg, i.v.) and increases the discharge rate of 80% of mPFC pyramidal neurons in the same dose range (ED50=0.62 μg/kg, i.v.). Both effects are reversed by the subsequent administration of the 5-HT1A receptor antagonist (±)WAY100635. In microdialysis studies, Befiradol (F13640; NLX-112) (0.04-0.63 mg/kg, i.p.) dose-dependently decreases extracellular 5-HT in the hippocampus and mPFC. Likewise, Befiradol (F13640; NLX-112) (0.01-2.5 mg/kg, i.p.) dose-dependently increases extracellular DA in mPFC, an effect dependent on the activation of postsynaptic 5-HT1A receptors in mPFC. Local perfusion of Befiradol in mPFC (1-1,000 μM) also increases extracellular DA in a concentration-dependent manner. Both the systemic and local effects of Befiradol are prevented by prior (±)WAY100635 administration[1].

[1]. Lladó-Pelfort L, et al. In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat. Psychopharmacology (Berl). 2012 May;221(2):261-72.

Protocol of Befiradol hydrochloride (NLX-112 (hydrochloride))

Animal experiment:

Rats[1]Male albino Wistar rats (230-300 g) are used throughout the study. Rats are anaesthetized with chloral hydrate (400-500 mg/kg, i.p.) or isoflurane. For the experiment with systemic administration of the compounds, saline or (±)WAY100635 are injected s.c., followed, 40 min later, by i.p. administration of saline or Befiradol. For the experiments with local perfusion, saline is injected s.c. and 40 min later, Befiradol (F13640; NLX-112) is added to the perfusion medium for the concentration-response experiment. For the antagonism, (±)WAY100635 (or aCSF) is delivered through the dialysis probe and 40 min later, Befiradol is added to the perfusion medium. Samples are collected for 140 min after administration or beginning of the perfusion of the agonist[1].

References:

[1]. Lladó-Pelfort L, et al. In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat. Psychopharmacology (Berl). 2012 May;221(2):261-72.

Chemical Properties of Befiradol hydrochloride (NLX-112 (hydrochloride))

Cas No. SDF
Canonical SMILES O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=C3)(F)CC2.Cl
Formula C20H23Cl2F2N3O M.Wt 430.32
الذوبان DMSO : 125 mg/mL (290.48 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Befiradol hydrochloride (NLX-112 (hydrochloride))

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3239 mL 11.6193 mL 23.2385 mL
5 mM 0.4648 mL 2.3239 mL 4.6477 mL
10 mM 0.2324 mL 1.1619 mL 2.3239 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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