The biochemical and cellular changes that occur following administration of 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP) are remarkably similar to that seen in idiopathic Parkinson's disease (PD). In this review, we detail the molecular activities of this compound from peripheral intoxication through its various biotransformations. In addition, we detail the interplay that occurs between the different cellular compartments (neurons and glia) that eventually consort to kill substantia nigra pars compacta (SNpc) neurons.