1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Befiradol hydrochloride (Synonyms: NLX-112 (hydrochloride); F 13640 (hydrochloride))

Cat. No.: HY-14785A
Handling Instructions

Befiradol hydrochloride is a selective 5-HT1A receptor agonist.

For research use only. We do not sell to patients.

Befiradol hydrochloride Chemical Structure

Befiradol hydrochloride Chemical Structure

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Other Forms of Befiradol hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Befiradol hydrochloride is a selective 5-HT1A receptor agonist.

IC50 & Target

5-HT1A receptor[1].

In Vivo

Befiradol (F13640) 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 (0.04-0.63 mg/kg, i.p.) dose-dependently decreases extracellular 5-HT in the hippocampus and mPFC. Likewise, Befiradol (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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

430.32

Formula

C₂₀H₂₃Cl₂F₂N₃O

SMILES

O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=C3)(F)CC2.Cl

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Befiradol hydrochloride
Cat. No.:
HY-14785A
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Befiradol hydrochloride

Cat. No.: HY-14785A