Neuroprotective effects of the novel D3/D2 receptor agonist and antiparkinson agent, S32504, in vitro against 1-methyl-4-phenylpyridinium (MPP+) and in vivo against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP): a comparison to ropinirole

S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2 Receptors: II. Actions in Rodent, Primate, and Cellular Models of Antiparkinsonian Activity in Comparison to Ropinirole

“…However, in the present model, it was only weakly active, confirming our earlier work (Joyce et al, 2003b) and an independent study of a mesencephalic cell line . Furthermore, in a parallel in vivo study, we recently showed (Joyce et al, 2003b) that S32504 is more potent and effective than ropinirole in mice in protecting nigrostriatal, dopaminergic neurones from the neurotoxic effects of MPTP.…”

“…Though transformed SH-SY5Y cells bear both D 3 and D 2 receptors (Joyce et al, 2003b), blockade of the neuroprotective actions of S32504 by raclopride and S33084, but not L741,626, suggests a principle role of the former. D 3 sites are similarly implicated in the neuroprotective effects of pramipexole both in this (J. Joyce and M. J. Millan, unpublished observations) and other ) cell lines.…”

S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2Receptors: I. Cellular, Electrophysiological, and Neurochemical Profile in Comparison with Ropinirole

“…The precise physiological significance of S32504-induced MAP kinase via hD 3 receptors remains to be clarified. However, this signal is jpet.aspetjournals.org implicated in the neuroprotective influence of S32504 and other dopaminergic agonists upon dopaminergic neurons that, as discussed in the accompanying paper (Millan et al, 2004b) and elsewhere (Joyce et al, 2003;Ramirez et al, 2003), appear to involve the activation of dopamine D 3 receptors.…”

“…The role of D 3 compared with D 2 receptors in the neuroprotective properties of dopaminergic agonists in Parkinson's patients (Whone et al, 2003) also remains unclear. Nevertheless, as discussed in the accompanying paper (Millan et al, 2004b), D 3 sites participate in the ability of dopamine D 3 /D 2 receptor agonists to protect dopaminergic neurons from neurotoxic damage in rodents (Joyce et al, 2003;Ramirez et al, 2003).…”

An Efficient Synthesis of 3,4-Dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine Derivatives Catalyzed by Zirconyl(IV) Chloride and Evaluation of its Biological Activities

“…In addition, naphthoxazine derivatives have exhibited therapeutic potential for the treatment of Parkinson's disease. 8,9 Multicomponent reactions (MCRs), defined as one pot reactions in which at least three functional groups join through covalent bonds, have been steadily gaining importance in synthetic organic chemistry. [10][11][12][13] The reagents employed may be different molecules or they may be different functional groups of the same reagent.…”