135354-02-8
Chemical Structure
Xaliproden free base
Synonym(s): SR57746A free base
- CAS No.: 135354-02-8
- Formula:C24H22F3N
- Molecular Weight:381.43
IUPAC Name: 1-(2-(naphthalen-2-yl)ethyl)-4-(3-(trifluoromethyl)phenyl)-1,2,3,6-tetrahydropyridine
InChIKey: WJJYZXPHLSLMGE-UHFFFAOYSA-N
SMILES: FC(F)(F)C1=CC(C2=CCN(CC2)CCC3=CC=C4C=CC=CC4=C3)=CC=C1
Biological Activity: Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety[1][2][3][4].
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Xaliproden free base | Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety. | |||||||||||||||||||||
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References
- [1]. Appert-Collin A, et al. Xaliproden (SR57746A) induces 5-HT1A receptor-mediated MAP kinase activation in PC12 cells. Int J Immunopathol Pharmacol. 2005;18(2):233-244. [Content Brief]
- [2]. Lee HJ, et al. Xaliproden improves diabetic kidney disease through JNK-mediated renal tubular protection. Biochem Pharmacol. Published online March 22, 2026. [Content Brief]
- [3]. Andoh T, et al. Effects of xaliproden, a 5-HT₁A agonist, on mechanical allodynia caused by chemotherapeutic agents in mice. Eur J Pharmacol. 2013;721(1-3):231-236. [Content Brief]
- [4]. Martel JC, et al. 5-HT1A receptors are involved in the effects of xaliproden on G-protein activation, neurotransmitter release and nociception. Br J Pharmacol. 2009;158(1):232-242. [Content Brief]
