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
Identifieur interne : 000613 ( PascalFrancis/Curation ); précédent : 000612; suivant : 000614Neuroprotective 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
Auteurs : Jeffrey N. Joyce [États-Unis] ; Steve Presgraves [États-Unis] ; Lynn Renish [États-Unis] ; Sabinne Borwege [États-Unis] ; Tracy Osredkar [États-Unis] ; Diane Hagner [États-Unis] ; Maria Replogle [États-Unis] ; Mateo Pazsoldan [États-Unis] ; Mark J. Millan [France]Source :
- Experimental neurology : (Print) [ 0014-4886 ] ; 2003.
Descripteurs français
- Pascal (Inist)
- Parkinson maladie, Récepteur dopaminergique D3, Récepteur dopaminergique D2, Système nerveux pathologie, Antiparkinsonien, In vitro, Etude comparative, Ropinirole, Dérivée, Animal, Primates, Modèle, Pramipexole, Mort cellulaire, Subchronique, Traitement, Souris, Tyrosine 3-monooxygenase, Locus niger, Aire tegmentaire ventrale, Dose forte.
English descriptors
- KwdEn :
- Animal, Antiparkinson agent, Cell death, Comparative study, D2 Dopamine receptor, D3 Dopamine receptor, Derivative, High dose, In vitro, Locus niger, Models, Mouse, Nervous system diseases, Parkinson disease, Pramipexole, Primates, Ropinirole, Subchronic, Treatment, Tyrosine 3-monooxygenase, Ventral tegmental area.
Abstract
The novel naphtoxazine derivative and preferential D, vs D2 receptor agonist, S32504, restores perturbed motor function in rodent and primate models of antiparkinsonian activity with a potency superior to those of two further, preferential D, receptor agonists, pramipexole and ropinirole. However, potential neuroprotective properties of S32054 have not, to date, been evaluated. Herein, employing several measures of cellular integrity, we demonstrate that S32504 robustly, concentration-dependently and completely protects terminally differentiated SH-SYSY cells against 1-methyl-4-phenylpyridinium (MPP+)-induced cell death in vitro. Further, S32504 was substantially more potent than pramipexole and ropinirole, the latter of which was neurotoxic at high concentrations. In vivo, subchronic treatment with low (0.25 mg/kg) and high (2.5 mg/kg) doses of S32504 prior to and during treatment of mice with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP, provided complete protection against MPTP-induced tyrosine hydroxylase immunoreactive (TH-IR) neuronal death in the substantia nigra pars compacta and ventral tegmental area. A high dose of ropinirole (2.5 mg/kg) provided some protection but statistical significance was not attained, and a low dose (0.25 mg/kg) was ineffective. Neither drug afforded protection against the MPTP-induced loss of DA fibers in the striatum, as measured by TH-IR and dopamine transporter immunoreactive fiber counts. In conclusion, the novel naphotoxazine and dopaminergic agonist, S32504, robustly protects dopaminergic neurones against the neurotoxic effects of MPP+ and MPTP in in vitro and in vivo models, respectively. The underlying mechanisms and therapeutic pertinence of these actions will be of interest to further evaluate in view of its potent actions in behavioral models of antiparkinson activity.
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<front><div type="abstract" xml:lang="en">The novel naphtoxazine derivative and preferential D, vs D<sub>2</sub>
receptor agonist, S32504, restores perturbed motor function in rodent and primate models of antiparkinsonian activity with a potency superior to those of two further, preferential D, receptor agonists, pramipexole and ropinirole. However, potential neuroprotective properties of S32054 have not, to date, been evaluated. Herein, employing several measures of cellular integrity, we demonstrate that S32504 robustly, concentration-dependently and completely protects terminally differentiated SH-SYSY cells against 1-methyl-4-phenylpyridinium (MPP+)-induced cell death in vitro. Further, S32504 was substantially more potent than pramipexole and ropinirole, the latter of which was neurotoxic at high concentrations. In vivo, subchronic treatment with low (0.25 mg/kg) and high (2.5 mg/kg) doses of S32504 prior to and during treatment of mice with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP, provided complete protection against MPTP-induced tyrosine hydroxylase immunoreactive (TH-IR) neuronal death in the substantia nigra pars compacta and ventral tegmental area. A high dose of ropinirole (2.5 mg/kg) provided some protection but statistical significance was not attained, and a low dose (0.25 mg/kg) was ineffective. Neither drug afforded protection against the MPTP-induced loss of DA fibers in the striatum, as measured by TH-IR and dopamine transporter immunoreactive fiber counts. In conclusion, the novel naphotoxazine and dopaminergic agonist, S32504, robustly protects dopaminergic neurones against the neurotoxic effects of MPP<sup>+</sup>
and MPTP in in vitro and in vivo models, respectively. The underlying mechanisms and therapeutic pertinence of these actions will be of interest to further evaluate in view of its potent actions in behavioral models of antiparkinson activity.</div>
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<fA43 i1="01"><s1>INIST</s1>
<s2>9181</s2>
<s5>354000118845000410</s5>
</fA43>
<fA44><s0>0000</s0>
<s1>© 2004 INIST-CNRS. All rights reserved.</s1>
</fA44>
<fA45><s0>2 p.1/4</s0>
</fA45>
<fA47 i1="01" i2="1"><s0>04-0276961</s0>
</fA47>
<fA60><s1>P</s1>
</fA60>
<fA61><s0>A</s0>
</fA61>
<fA64 i1="01" i2="1"><s0>Experimental neurology : (Print)</s0>
</fA64>
<fA66 i1="01"><s0>USA</s0>
</fA66>
<fC01 i1="01" l="ENG"><s0>The novel naphtoxazine derivative and preferential D, vs D<sub>2</sub>
receptor agonist, S32504, restores perturbed motor function in rodent and primate models of antiparkinsonian activity with a potency superior to those of two further, preferential D, receptor agonists, pramipexole and ropinirole. However, potential neuroprotective properties of S32054 have not, to date, been evaluated. Herein, employing several measures of cellular integrity, we demonstrate that S32504 robustly, concentration-dependently and completely protects terminally differentiated SH-SYSY cells against 1-methyl-4-phenylpyridinium (MPP+)-induced cell death in vitro. Further, S32504 was substantially more potent than pramipexole and ropinirole, the latter of which was neurotoxic at high concentrations. In vivo, subchronic treatment with low (0.25 mg/kg) and high (2.5 mg/kg) doses of S32504 prior to and during treatment of mice with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP, provided complete protection against MPTP-induced tyrosine hydroxylase immunoreactive (TH-IR) neuronal death in the substantia nigra pars compacta and ventral tegmental area. A high dose of ropinirole (2.5 mg/kg) provided some protection but statistical significance was not attained, and a low dose (0.25 mg/kg) was ineffective. Neither drug afforded protection against the MPTP-induced loss of DA fibers in the striatum, as measured by TH-IR and dopamine transporter immunoreactive fiber counts. In conclusion, the novel naphotoxazine and dopaminergic agonist, S32504, robustly protects dopaminergic neurones against the neurotoxic effects of MPP<sup>+</sup>
and MPTP in in vitro and in vivo models, respectively. The underlying mechanisms and therapeutic pertinence of these actions will be of interest to further evaluate in view of its potent actions in behavioral models of antiparkinson activity.</s0>
</fC01>
<fC02 i1="01" i2="X"><s0>002B17</s0>
</fC02>
<fC03 i1="01" i2="X" l="FRE"><s0>Parkinson maladie</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="ENG"><s0>Parkinson disease</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="SPA"><s0>Parkinson enfermedad</s0>
<s5>01</s5>
</fC03>
<fC03 i1="02" i2="X" l="FRE"><s0>Récepteur dopaminergique D3</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="ENG"><s0>D3 Dopamine receptor</s0>
<s5>02</s5>
<s6>«D3» Dopamine receptor</s6>
</fC03>
<fC03 i1="02" i2="X" l="SPA"><s0>Receptor dopaminérgico D3</s0>
<s5>02</s5>
</fC03>
<fC03 i1="03" i2="X" l="FRE"><s0>Récepteur dopaminergique D2</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="ENG"><s0>D2 Dopamine receptor</s0>
<s5>03</s5>
<s6>«D2» Dopamine receptor</s6>
</fC03>
<fC03 i1="03" i2="X" l="SPA"><s0>Receptor dopaminérgico D2</s0>
<s5>03</s5>
</fC03>
<fC03 i1="04" i2="X" l="FRE"><s0>Système nerveux pathologie</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="ENG"><s0>Nervous system diseases</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="SPA"><s0>Sistema nervioso patología</s0>
<s5>04</s5>
</fC03>
<fC03 i1="05" i2="X" l="FRE"><s0>Antiparkinsonien</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="ENG"><s0>Antiparkinson agent</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="SPA"><s0>Antiparkinsoniano</s0>
<s5>05</s5>
</fC03>
<fC03 i1="06" i2="X" l="FRE"><s0>In vitro</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG"><s0>In vitro</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="SPA"><s0>In vitro</s0>
<s5>06</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE"><s0>Etude comparative</s0>
<s5>08</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG"><s0>Comparative study</s0>
<s5>08</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA"><s0>Estudio comparativo</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE"><s0>Ropinirole</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>09</s5>
</fC03>
<fC03 i1="08" i2="X" l="ENG"><s0>Ropinirole</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>09</s5>
</fC03>
<fC03 i1="08" i2="X" l="SPA"><s0>Ropinirol</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="FRE"><s0>Dérivée</s0>
<s5>11</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG"><s0>Derivative</s0>
<s5>11</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA"><s0>Derivada</s0>
<s5>11</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE"><s0>Animal</s0>
<s5>12</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG"><s0>Animal</s0>
<s5>12</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA"><s0>Animal</s0>
<s5>12</s5>
</fC03>
<fC03 i1="11" i2="X" l="FRE"><s0>Primates</s0>
<s2>NS</s2>
<s5>14</s5>
</fC03>
<fC03 i1="11" i2="X" l="ENG"><s0>Primates</s0>
<s2>NS</s2>
<s5>14</s5>
</fC03>
<fC03 i1="11" i2="X" l="SPA"><s0>Primates</s0>
<s2>NS</s2>
<s5>14</s5>
</fC03>
<fC03 i1="12" i2="X" l="FRE"><s0>Modèle</s0>
<s5>15</s5>
</fC03>
<fC03 i1="12" i2="X" l="ENG"><s0>Models</s0>
<s5>15</s5>
</fC03>
<fC03 i1="12" i2="X" l="SPA"><s0>Modelo</s0>
<s5>15</s5>
</fC03>
<fC03 i1="13" i2="X" l="FRE"><s0>Pramipexole</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>17</s5>
</fC03>
<fC03 i1="13" i2="X" l="ENG"><s0>Pramipexole</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>17</s5>
</fC03>
<fC03 i1="13" i2="X" l="SPA"><s0>Pramipexol</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>17</s5>
</fC03>
<fC03 i1="14" i2="X" l="FRE"><s0>Mort cellulaire</s0>
<s5>18</s5>
</fC03>
<fC03 i1="14" i2="X" l="ENG"><s0>Cell death</s0>
<s5>18</s5>
</fC03>
<fC03 i1="14" i2="X" l="SPA"><s0>Muerte celular</s0>
<s5>18</s5>
</fC03>
<fC03 i1="15" i2="X" l="FRE"><s0>Subchronique</s0>
<s5>19</s5>
</fC03>
<fC03 i1="15" i2="X" l="ENG"><s0>Subchronic</s0>
<s5>19</s5>
</fC03>
<fC03 i1="15" i2="X" l="SPA"><s0>Subcrónico</s0>
<s5>19</s5>
</fC03>
<fC03 i1="16" i2="X" l="FRE"><s0>Traitement</s0>
<s5>20</s5>
</fC03>
<fC03 i1="16" i2="X" l="ENG"><s0>Treatment</s0>
<s5>20</s5>
</fC03>
<fC03 i1="16" i2="X" l="SPA"><s0>Tratamiento</s0>
<s5>20</s5>
</fC03>
<fC03 i1="17" i2="X" l="FRE"><s0>Souris</s0>
<s5>21</s5>
</fC03>
<fC03 i1="17" i2="X" l="ENG"><s0>Mouse</s0>
<s5>21</s5>
</fC03>
<fC03 i1="17" i2="X" l="SPA"><s0>Ratón</s0>
<s5>21</s5>
</fC03>
<fC03 i1="18" i2="X" l="FRE"><s0>Tyrosine 3-monooxygenase</s0>
<s2>FE</s2>
<s5>22</s5>
<s6>Tyrosine «3»-monooxygenase</s6>
</fC03>
<fC03 i1="18" i2="X" l="ENG"><s0>Tyrosine 3-monooxygenase</s0>
<s2>FE</s2>
<s5>22</s5>
<s6>Tyrosine «3»-monooxygenase</s6>
</fC03>
<fC03 i1="18" i2="X" l="SPA"><s0>Tyrosine 3-monooxygenase</s0>
<s2>FE</s2>
<s5>22</s5>
<s6>Tyrosine «3»-monooxygenase</s6>
</fC03>
<fC03 i1="19" i2="X" l="FRE"><s0>Locus niger</s0>
<s5>23</s5>
</fC03>
<fC03 i1="19" i2="X" l="ENG"><s0>Locus niger</s0>
<s5>23</s5>
</fC03>
<fC03 i1="19" i2="X" l="SPA"><s0>Locus níger</s0>
<s5>23</s5>
</fC03>
<fC03 i1="20" i2="X" l="FRE"><s0>Aire tegmentaire ventrale</s0>
<s5>24</s5>
</fC03>
<fC03 i1="20" i2="X" l="ENG"><s0>Ventral tegmental area</s0>
<s5>24</s5>
</fC03>
<fC03 i1="20" i2="X" l="SPA"><s0>Area tegmental ventral</s0>
<s5>24</s5>
</fC03>
<fC03 i1="21" i2="X" l="FRE"><s0>Dose forte</s0>
<s5>35</s5>
</fC03>
<fC03 i1="21" i2="X" l="ENG"><s0>High dose</s0>
<s5>35</s5>
</fC03>
<fC03 i1="21" i2="X" l="SPA"><s0>Dosis fuerte</s0>
<s5>35</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="01" i2="X" l="ENG"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="01" i2="X" l="SPA"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="FRE"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="ENG"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="02" i2="X" l="SPA"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="FRE"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="ENG"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="03" i2="X" l="SPA"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="04" i2="X" l="FRE"><s0>Oxidoreductases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="04" i2="X" l="ENG"><s0>Oxidoreductases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="04" i2="X" l="SPA"><s0>Oxidoreductases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="05" i2="X" l="FRE"><s0>Enzyme</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="05" i2="X" l="ENG"><s0>Enzyme</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="05" i2="X" l="SPA"><s0>Enzima</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="06" i2="X" l="FRE"><s0>Encéphale pathologie</s0>
<s5>37</s5>
</fC07>
<fC07 i1="06" i2="X" l="ENG"><s0>Cerebral disorder</s0>
<s5>37</s5>
</fC07>
<fC07 i1="06" i2="X" l="SPA"><s0>Encéfalo patología</s0>
<s5>37</s5>
</fC07>
<fC07 i1="07" i2="X" l="FRE"><s0>Système nerveux central</s0>
<s5>38</s5>
</fC07>
<fC07 i1="07" i2="X" l="ENG"><s0>Central nervous system</s0>
<s5>38</s5>
</fC07>
<fC07 i1="07" i2="X" l="SPA"><s0>Sistema nervioso central</s0>
<s5>38</s5>
</fC07>
<fC07 i1="08" i2="X" l="FRE"><s0>Catécholamine</s0>
<s5>39</s5>
</fC07>
<fC07 i1="08" i2="X" l="ENG"><s0>Catecholamine</s0>
<s5>39</s5>
</fC07>
<fC07 i1="08" i2="X" l="SPA"><s0>Catecolamina</s0>
<s5>39</s5>
</fC07>
<fC07 i1="09" i2="X" l="FRE"><s0>Neurotransmetteur</s0>
<s5>40</s5>
</fC07>
<fC07 i1="09" i2="X" l="ENG"><s0>Neurotransmitter</s0>
<s5>40</s5>
</fC07>
<fC07 i1="09" i2="X" l="SPA"><s0>Neurotransmisor</s0>
<s5>40</s5>
</fC07>
<fC07 i1="10" i2="X" l="FRE"><s0>Extrapyramidal syndrome</s0>
<s5>41</s5>
</fC07>
<fC07 i1="10" i2="X" l="ENG"><s0>Extrapyramidal syndrome</s0>
<s5>41</s5>
</fC07>
<fC07 i1="10" i2="X" l="SPA"><s0>Extrapiramidal síndrome</s0>
<s5>41</s5>
</fC07>
<fC07 i1="11" i2="X" l="FRE"><s0>Maladie dégénérative</s0>
<s5>42</s5>
</fC07>
<fC07 i1="11" i2="X" l="ENG"><s0>Degenerative disease</s0>
<s5>42</s5>
</fC07>
<fC07 i1="11" i2="X" l="SPA"><s0>Enfermedad degenerativa</s0>
<s5>42</s5>
</fC07>
<fC07 i1="12" i2="X" l="FRE"><s0>Système nerveux central pathologie</s0>
<s5>43</s5>
</fC07>
<fC07 i1="12" i2="X" l="ENG"><s0>Central nervous system disease</s0>
<s5>43</s5>
</fC07>
<fC07 i1="12" i2="X" l="SPA"><s0>Sistema nervosio central patología</s0>
<s5>43</s5>
</fC07>
<fN21><s1>173</s1>
</fN21>
<fN44 i1="01"><s1>OTO</s1>
</fN44>
<fN82><s1>OTO</s1>
</fN82>
</pA>
</standard>
</inist>
</record>
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{{Explor lien |wiki= Wicri/Sante |area= ParkinsonFranceV1 |flux= PascalFrancis |étape= Curation |type= RBID |clé= Pascal:04-0276961 |texte= 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 }}
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