1.The neuroprotective effect of talipexole from paraquat-induced cell death in dopaminergic neuronal cells.
Gómez-Sánchez R1, Bravo-San Pedro JM, Niso-Santano M, Soler G, Fuentes JM, González-Polo RA. Neurotoxicology. 2010 Dec;31(6):701-8. doi: 10.1016/j.neuro.2010.07.005. Epub 2010 Jul 29.
Talipexole is a non-ergot dopamine (DA) agonist that has been used in the treatment of Parkinson's disease. In the present study, we examined the effect of talipexole on paraquat (PQ)-induced N27 cell death and the intracellular pathways involved in this effect. Pretreatment of N27 cells with talipexole (1mM) resulted in significant protection against paraquat-induced cell death. In N27 cells, talipexole inhibited paraquat-induced apoptotic hallmarks such as cytochrome c release, caspase-3 activation, chromatin condensation and externalization of phosphatidilserine. Talipexole pretreatment prevents the reduction in the anti-apoptotic Bcl-x(L) protein and increases in the pro-apoptotic form of Bak and p-Bad, both induced by PQ. Finally, we also observed that talipexole abrogates the activation of cell death pathways JNK1/2 and p38 produced by PQ, and increases the phosphorylated (active) forms of the pro-survival pathways ERK1/2 and Akt. These results reveal that talipexole exerts a neuroprotective effect in a mesencephalic cell line exposed to the neurotoxin PQ, which is related to the etiology of Parkinson's disease.
2.Pharmacokinetic profile of talipexole in healthy volunteers is not altered when it is co-administered with Madopar (co-beneldopa).
Zhang TT1, Song M, Hang TJ, Xu XF, Wen AD, Yang L, Jia L. J Clin Pharm Ther. 2009 Jun;34(3):345-54. doi: 10.1111/j.1365-2710.2008.01008.x.
OBJECTIVES: To investigate the pharmacokinetics of talipexole hydrochloride tablets and the potential influence of Madopar (benserazide and levodopa combination; co-beneldopa) tablets on talipexole's pharmacokinetics when the two tablets are co-administered orally to healthy Chinese volunteers.