Befiradol hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Befiradol hydrochloride (NLX-112 hydrochloride) 是选择性的5-羟色胺 1A (5-HT)1A 受体激动剂。

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

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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.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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2436760-81-3

430.32

C20H23Cl2F2N3O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (290.48 mM; 超声助溶 )

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

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(-20℃)

With Ice Pack

≥ 2 years