Xaliproden (hydrochloride)

Xaliproden is an agonist of the serotonin (5-HT) receptor subtype 5-HT_1A (IC₅₀ = 4.3 nM in a radioligand binding assay).¹ It is selective for 5-HT_1A over 5-HT₂ and α₁-adrenergic receptors (IC₅₀s = 697 and 630 nM, respectively), as well as a panel of 13 additional neurotransmitter receptors and ion channels (IC₅₀s = ≥10 µM for all) but also binds sigma (σ) receptors (IC₅₀ = 73 nM). Xaliproden (250 nM) increases NGF-induced neurite outgrowth and α-actinin levels in PC12 cells.² It decreases hippocampal neuronal damage and reduces impairments in sensorimotor function in rat models of transient global ischemia induced by four-vessel occlusion (4-VO) and sciatic nerve crush injury, respectively, when administered at a dose of 10 mg/kg per day.³ Xaliproden (10 mg/kg per day) inhibits CNS mononuclear cell infiltration and increases in cerebrospinal fluid IgG levels in a rat model of experimental autoimmune encephalomyelitis (EAE) induced by myelin basic protein.⁴

WARNING This product is not for human or veterinary use.

1. Bachy, A., Steinberg, R., Santucci, V., et al. Biochemical and electrophysiological properties of SR 57746A, a new, potent 5-HT_1A receptor agonist. Fundam. Clin. Pharmacol. 7(9), 487-497 (1993).

2. Pradines, A., Magazin, M., Schlitz, P., et al. Evidence for nerve growth factor-potentiating activities of the nonpeptidic compound SR 57746A in PC12 cells. J. Neurochem. 64(5), 1954-1964 (1995).

3. Fournier, J., Steinberg, R., Gauthier, T., et al. Protective effects of SR 57746A in central and peripheral models of neurodegenerative disorders in rodents and primates. Neuroscience 55(3), 629-641 (1993).

4. Bourrié, B., Bribes, E., Esclangon, M., et al. The neuroprotective agent SR 57746A abrogates experimental autoimmune encephalomyelitis and impairs associated blood-brain barrier disruption: Implications for multiple sclerosis treatment. Proc. Natl. Acad. Sci. USA 96(22), 12855-12859 (1999).