MIF-1 and its peptidomimetic analogs attenuate haloperidol-induced vacuous chewing movements and modulate apomorphine-induced rotational behavior in 6-hydroxydopamine-lesioned rats
Identifieur interne : 000706 ( PascalFrancis/Corpus ); précédent : 000705; suivant : 000707MIF-1 and its peptidomimetic analogs attenuate haloperidol-induced vacuous chewing movements and modulate apomorphine-induced rotational behavior in 6-hydroxydopamine-lesioned rats
Auteurs : Jessica M. Castellano ; Jody Batrynchuk ; Kristine Dolbeare ; Vaneeta Verma ; Amandeep Mann ; Kevin J. Skoblenick ; Rodney L. Johnson ; Ram K. MishraSource :
- Peptides : (New York, NY. 1980) [ 0196-9781 ] ; 2007.
Descripteurs français
- Pascal (Inist)
English descriptors
- KwdEn :
Abstract
Two melanocyte-stimulating hormone release inhibiting factor-1 (MIF-1) also known as L-prolyl-L-leucyl-glycinamide (PLG) peptidomimetic analogs, 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]-amino] -3-(butyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (A) and 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]amino]-3-(benzyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (B), were evaluated for their ability to modulate dopaminergic activity by measuring apomorphine-induced rotations in 6-hydroxydopamine (6-OHDA)-lesioned rats, and haloperidol (HP)-induced vacuous chewing movements (VCMs) in rats; animal models of Parkinson's disease (PD) and human tardive dyskinesia (TD), respectively. In the 6-OHDA model, both analogs were found to potentiate the contralateral rotational behavior induced by apomorphine dose-dependently and with approximately the same potency. Furthermore, each analog was able to significantly attenuate HP-induced VCMs with almost equal efficacy. The potency and efficacy of these analogs were significantly greater than their parent compound, PLG. These results suggest that both analogs can modulate dopaminergic activity in vivo, likely by the same mechanisms recruited by PLG previously reported.
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Pour connaître la documentation sur le format Inist Standard.
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Format Inist (serveur)
NO : | PASCAL 07-0480619 INIST |
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ET : | MIF-1 and its peptidomimetic analogs attenuate haloperidol-induced vacuous chewing movements and modulate apomorphine-induced rotational behavior in 6-hydroxydopamine-lesioned rats |
AU : | CASTELLANO (Jessica M.); BATRYNCHUK (Jody); DOLBEARE (Kristine); VERMA (Vaneeta); MANN (Amandeep); SKOBLENICK (Kevin J.); JOHNSON (Rodney L.); MISHRA (Ram K.) |
AF : | Department of Psychiatry and Behavioral Neurosciences, McMaster University, 1200 Main Street West/Hamilton, Ontario, L8N 3Z5/Canada (1 aut., 2 aut., 4 aut., 5 aut., 6 aut., 8 aut.); Department of Medicinal Chemistry, University of Minnesota/Minneapolis, MN 55455/Etats-Unis (3 aut., 7 aut.) |
DT : | Publication en série; Niveau analytique |
SO : | Peptides : (New York, NY. 1980); ISSN 0196-9781; Coden PPTDD5; Etats-Unis; Da. 2007; Vol. 28; No. 10; Pp. 2009-2015; Bibl. 52 ref. |
LA : | Anglais |
EA : | Two melanocyte-stimulating hormone release inhibiting factor-1 (MIF-1) also known as L-prolyl-L-leucyl-glycinamide (PLG) peptidomimetic analogs, 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]-a mino] -3-(butyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (A) and 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]amino]-3-(benzyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (B), were evaluated for their ability to modulate dopaminergic activity by measuring apomorphine-induced rotations in 6-hydroxydopamine (6-OHDA)-lesioned rats, and haloperidol (HP)-induced vacuous chewing movements (VCMs) in rats; animal models of Parkinson's disease (PD) and human tardive dyskinesia (TD), respectively. In the 6-OHDA model, both analogs were found to potentiate the contralateral rotational behavior induced by apomorphine dose-dependently and with approximately the same potency. Furthermore, each analog was able to significantly attenuate HP-induced VCMs with almost equal efficacy. The potency and efficacy of these analogs were significantly greater than their parent compound, PLG. These results suggest that both analogs can modulate dopaminergic activity in vivo, likely by the same mechanisms recruited by PLG previously reported. |
CC : | 002A28; 002B17G; 002B17A01; 002B02B03 |
FD : | Analogue; Halopéridol; Mastication; Apomorphine; Comportement; Oxidopamine; Parkinson maladie; Animal; Contrôle moteur; Dyskinésie; Lésion; Dopamine; MSH; Libération; Rat |
FG : | Psychotrope; Neuroleptique; Antagoniste dopamine; Butyrophénone dérivé; Récepteur dopaminergique D2; Agoniste; Récepteur dopaminergique D1; Stimulant dopaminergique; Récepteur adrénergique; Sympathomimétique; Catécholamine; Neurotransmetteur; Hormone hypophysaire; Encéphale pathologie; Extrapyramidal syndrome; Maladie dégénérative; Système nerveux central pathologie; Système nerveux pathologie; Mouvement involontaire; Trouble neurologique; Rodentia; Mammalia; Vertebrata |
ED : | Analog; Haloperidol; Chewing; Behavior; Oxidopamine; Parkinson disease; Animal; Motor control; Dyskinesia; Lesion; Dopamine; Melanocyte stimulating hormone; Release; Rat |
EG : | Psychotropic; Neuroleptic; Dopamine antagonist; Butyrophenone derivatives; D2 Dopamine receptor; Agonist; D1 Dopamine receptor; Dopamine agonist; Adrenergic receptor; Sympathomimetic; Catecholamine; Neurotransmitter; Pituitary hormone; Cerebral disorder; Extrapyramidal syndrome; Degenerative disease; Central nervous system disease; Nervous system diseases; Involuntary movement; Neurological disorder; Rodentia; Mammalia; Vertebrata |
SD : | Análogo; Haloperidol; Masticación; Conducta; Oxidopamina; Parkinson enfermedad; Animal; Control motor; Disquinesia; Lesión; Dopamina; MSH; Liberación; Rata |
LO : | INIST-19060.354000149842240110 |
ID : | 07-0480619 |
Links to Exploration step
Pascal:07-0480619Le document en format XML
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Analog</term>
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<term>Behavior</term>
<term>Chewing</term>
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<term>Dyskinesia</term>
<term>Haloperidol</term>
<term>Lesion</term>
<term>Melanocyte stimulating hormone</term>
<term>Motor control</term>
<term>Oxidopamine</term>
<term>Parkinson disease</term>
<term>Rat</term>
<term>Release</term>
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<keywords scheme="Pascal" xml:lang="fr"><term>Analogue</term>
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<term>Oxidopamine</term>
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<term>Contrôle moteur</term>
<term>Dyskinésie</term>
<term>Lésion</term>
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<front><div type="abstract" xml:lang="en">Two melanocyte-stimulating hormone release inhibiting factor-1 (MIF-1) also known as L-prolyl-L-leucyl-glycinamide (PLG) peptidomimetic analogs, 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]-amino] -3-(butyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (A) and 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]amino]-3-(benzyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (B), were evaluated for their ability to modulate dopaminergic activity by measuring apomorphine-induced rotations in 6-hydroxydopamine (6-OHDA)-lesioned rats, and haloperidol (HP)-induced vacuous chewing movements (VCMs) in rats; animal models of Parkinson's disease (PD) and human tardive dyskinesia (TD), respectively. In the 6-OHDA model, both analogs were found to potentiate the contralateral rotational behavior induced by apomorphine dose-dependently and with approximately the same potency. Furthermore, each analog was able to significantly attenuate HP-induced VCMs with almost equal efficacy. The potency and efficacy of these analogs were significantly greater than their parent compound, PLG. These results suggest that both analogs can modulate dopaminergic activity in vivo, likely by the same mechanisms recruited by PLG previously reported.</div>
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<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="SPA"><s0>Haloperidol</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>02</s5>
</fC03>
<fC03 i1="03" i2="X" l="FRE"><s0>Mastication</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="ENG"><s0>Chewing</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="SPA"><s0>Masticación</s0>
<s5>03</s5>
</fC03>
<fC03 i1="04" i2="X" l="FRE"><s0>Apomorphine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>04</s5>
</fC03>
<fC03 i1="05" i2="X" l="FRE"><s0>Comportement</s0>
<s5>07</s5>
</fC03>
<fC03 i1="05" i2="X" l="ENG"><s0>Behavior</s0>
<s5>07</s5>
</fC03>
<fC03 i1="05" i2="X" l="SPA"><s0>Conducta</s0>
<s5>07</s5>
</fC03>
<fC03 i1="06" i2="X" l="FRE"><s0>Oxidopamine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>08</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG"><s0>Oxidopamine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>08</s5>
</fC03>
<fC03 i1="06" i2="X" l="SPA"><s0>Oxidopamina</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>08</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE"><s0>Parkinson maladie</s0>
<s5>09</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG"><s0>Parkinson disease</s0>
<s5>09</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA"><s0>Parkinson enfermedad</s0>
<s5>09</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE"><s0>Animal</s0>
<s5>10</s5>
</fC03>
<fC03 i1="08" i2="X" l="ENG"><s0>Animal</s0>
<s5>10</s5>
</fC03>
<fC03 i1="08" i2="X" l="SPA"><s0>Animal</s0>
<s5>10</s5>
</fC03>
<fC03 i1="09" i2="X" l="FRE"><s0>Contrôle moteur</s0>
<s5>11</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG"><s0>Motor control</s0>
<s5>11</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA"><s0>Control motor</s0>
<s5>11</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE"><s0>Dyskinésie</s0>
<s5>12</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG"><s0>Dyskinesia</s0>
<s5>12</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA"><s0>Disquinesia</s0>
<s5>12</s5>
</fC03>
<fC03 i1="11" i2="X" l="FRE"><s0>Lésion</s0>
<s5>13</s5>
</fC03>
<fC03 i1="11" i2="X" l="ENG"><s0>Lesion</s0>
<s5>13</s5>
</fC03>
<fC03 i1="11" i2="X" l="SPA"><s0>Lesión</s0>
<s5>13</s5>
</fC03>
<fC03 i1="12" i2="X" l="FRE"><s0>Dopamine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>14</s5>
</fC03>
<fC03 i1="12" i2="X" l="ENG"><s0>Dopamine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>14</s5>
</fC03>
<fC03 i1="12" i2="X" l="SPA"><s0>Dopamina</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>14</s5>
</fC03>
<fC03 i1="13" i2="X" l="FRE"><s0>MSH</s0>
<s5>15</s5>
</fC03>
<fC03 i1="13" i2="X" l="ENG"><s0>Melanocyte stimulating hormone</s0>
<s5>15</s5>
</fC03>
<fC03 i1="13" i2="X" l="SPA"><s0>MSH</s0>
<s5>15</s5>
</fC03>
<fC03 i1="14" i2="X" l="FRE"><s0>Libération</s0>
<s5>16</s5>
</fC03>
<fC03 i1="14" i2="X" l="ENG"><s0>Release</s0>
<s5>16</s5>
</fC03>
<fC03 i1="14" i2="X" l="SPA"><s0>Liberación</s0>
<s5>16</s5>
</fC03>
<fC03 i1="15" i2="X" l="FRE"><s0>Rat</s0>
<s5>69</s5>
</fC03>
<fC03 i1="15" i2="X" l="ENG"><s0>Rat</s0>
<s5>69</s5>
</fC03>
<fC03 i1="15" i2="X" l="SPA"><s0>Rata</s0>
<s5>69</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE"><s0>Psychotrope</s0>
<s2>FX</s2>
<s5>20</s5>
</fC07>
<fC07 i1="01" i2="X" l="ENG"><s0>Psychotropic</s0>
<s2>FX</s2>
<s5>20</s5>
</fC07>
<fC07 i1="01" i2="X" l="SPA"><s0>Psicotropo</s0>
<s2>FX</s2>
<s5>20</s5>
</fC07>
<fC07 i1="02" i2="X" l="FRE"><s0>Neuroleptique</s0>
<s5>21</s5>
</fC07>
<fC07 i1="02" i2="X" l="ENG"><s0>Neuroleptic</s0>
<s5>21</s5>
</fC07>
<fC07 i1="02" i2="X" l="SPA"><s0>Neuroléptico</s0>
<s5>21</s5>
</fC07>
<fC07 i1="03" i2="X" l="FRE"><s0>Antagoniste dopamine</s0>
<s5>22</s5>
</fC07>
<fC07 i1="03" i2="X" l="ENG"><s0>Dopamine antagonist</s0>
<s5>22</s5>
</fC07>
<fC07 i1="03" i2="X" l="SPA"><s0>Antagonista dopamina</s0>
<s5>22</s5>
</fC07>
<fC07 i1="04" i2="X" l="FRE"><s0>Butyrophénone dérivé</s0>
<s5>23</s5>
</fC07>
<fC07 i1="04" i2="X" l="ENG"><s0>Butyrophenone derivatives</s0>
<s5>23</s5>
</fC07>
<fC07 i1="04" i2="X" l="SPA"><s0>Butirofenona derivado</s0>
<s5>23</s5>
</fC07>
<fC07 i1="05" i2="X" l="FRE"><s0>Récepteur dopaminergique D2</s0>
<s5>24</s5>
</fC07>
<fC07 i1="05" i2="X" l="ENG"><s0>D2 Dopamine receptor</s0>
<s5>24</s5>
<s6>«D2» Dopamine receptor</s6>
</fC07>
<fC07 i1="05" i2="X" l="SPA"><s0>Receptor dopaminérgico D2</s0>
<s5>24</s5>
</fC07>
<fC07 i1="06" i2="X" l="FRE"><s0>Agoniste</s0>
<s5>25</s5>
</fC07>
<fC07 i1="06" i2="X" l="ENG"><s0>Agonist</s0>
<s5>25</s5>
</fC07>
<fC07 i1="06" i2="X" l="SPA"><s0>Agonista</s0>
<s5>25</s5>
</fC07>
<fC07 i1="07" i2="X" l="FRE"><s0>Récepteur dopaminergique D1</s0>
<s5>26</s5>
</fC07>
<fC07 i1="07" i2="X" l="ENG"><s0>D1 Dopamine receptor</s0>
<s5>26</s5>
<s6>«D1» Dopamine receptor</s6>
</fC07>
<fC07 i1="07" i2="X" l="SPA"><s0>Receptor dopaminérgico D1</s0>
<s5>26</s5>
</fC07>
<fC07 i1="08" i2="X" l="FRE"><s0>Stimulant dopaminergique</s0>
<s5>27</s5>
</fC07>
<fC07 i1="08" i2="X" l="ENG"><s0>Dopamine agonist</s0>
<s5>27</s5>
</fC07>
<fC07 i1="08" i2="X" l="SPA"><s0>Estimulante dopaminérgico</s0>
<s5>27</s5>
</fC07>
<fC07 i1="09" i2="X" l="FRE"><s0>Récepteur adrénergique</s0>
<s5>28</s5>
</fC07>
<fC07 i1="09" i2="X" l="ENG"><s0>Adrenergic receptor</s0>
<s5>28</s5>
</fC07>
<fC07 i1="09" i2="X" l="SPA"><s0>Receptor adrenérgico</s0>
<s5>28</s5>
</fC07>
<fC07 i1="10" i2="X" l="FRE"><s0>Sympathomimétique</s0>
<s5>29</s5>
</fC07>
<fC07 i1="10" i2="X" l="ENG"><s0>Sympathomimetic</s0>
<s5>29</s5>
</fC07>
<fC07 i1="10" i2="X" l="SPA"><s0>Simpaticomimético</s0>
<s5>29</s5>
</fC07>
<fC07 i1="11" i2="X" l="FRE"><s0>Catécholamine</s0>
<s5>30</s5>
</fC07>
<fC07 i1="11" i2="X" l="ENG"><s0>Catecholamine</s0>
<s5>30</s5>
</fC07>
<fC07 i1="11" i2="X" l="SPA"><s0>Catecolamina</s0>
<s5>30</s5>
</fC07>
<fC07 i1="12" i2="X" l="FRE"><s0>Neurotransmetteur</s0>
<s5>31</s5>
</fC07>
<fC07 i1="12" i2="X" l="ENG"><s0>Neurotransmitter</s0>
<s5>31</s5>
</fC07>
<fC07 i1="12" i2="X" l="SPA"><s0>Neurotransmisor</s0>
<s5>31</s5>
</fC07>
<fC07 i1="13" i2="X" l="FRE"><s0>Hormone hypophysaire</s0>
<s5>38</s5>
</fC07>
<fC07 i1="13" i2="X" l="ENG"><s0>Pituitary hormone</s0>
<s5>38</s5>
</fC07>
<fC07 i1="13" i2="X" l="SPA"><s0>Hormona hipofisaria</s0>
<s5>38</s5>
</fC07>
<fC07 i1="14" i2="X" l="FRE"><s0>Encéphale pathologie</s0>
<s5>39</s5>
</fC07>
<fC07 i1="14" i2="X" l="ENG"><s0>Cerebral disorder</s0>
<s5>39</s5>
</fC07>
<fC07 i1="14" i2="X" l="SPA"><s0>Encéfalo patología</s0>
<s5>39</s5>
</fC07>
<fC07 i1="15" i2="X" l="FRE"><s0>Extrapyramidal syndrome</s0>
<s5>40</s5>
</fC07>
<fC07 i1="15" i2="X" l="ENG"><s0>Extrapyramidal syndrome</s0>
<s5>40</s5>
</fC07>
<fC07 i1="15" i2="X" l="SPA"><s0>Extrapiramidal síndrome</s0>
<s5>40</s5>
</fC07>
<fC07 i1="16" i2="X" l="FRE"><s0>Maladie dégénérative</s0>
<s5>41</s5>
</fC07>
<fC07 i1="16" i2="X" l="ENG"><s0>Degenerative disease</s0>
<s5>41</s5>
</fC07>
<fC07 i1="16" i2="X" l="SPA"><s0>Enfermedad degenerativa</s0>
<s5>41</s5>
</fC07>
<fC07 i1="17" i2="X" l="FRE"><s0>Système nerveux central pathologie</s0>
<s5>42</s5>
</fC07>
<fC07 i1="17" i2="X" l="ENG"><s0>Central nervous system disease</s0>
<s5>42</s5>
</fC07>
<fC07 i1="17" i2="X" l="SPA"><s0>Sistema nervosio central patología</s0>
<s5>42</s5>
</fC07>
<fC07 i1="18" i2="X" l="FRE"><s0>Système nerveux pathologie</s0>
<s5>43</s5>
</fC07>
<fC07 i1="18" i2="X" l="ENG"><s0>Nervous system diseases</s0>
<s5>43</s5>
</fC07>
<fC07 i1="18" i2="X" l="SPA"><s0>Sistema nervioso patología</s0>
<s5>43</s5>
</fC07>
<fC07 i1="19" i2="X" l="FRE"><s0>Mouvement involontaire</s0>
<s5>44</s5>
</fC07>
<fC07 i1="19" i2="X" l="ENG"><s0>Involuntary movement</s0>
<s5>44</s5>
</fC07>
<fC07 i1="19" i2="X" l="SPA"><s0>Movimiento involuntario</s0>
<s5>44</s5>
</fC07>
<fC07 i1="20" i2="X" l="FRE"><s0>Trouble neurologique</s0>
<s5>45</s5>
</fC07>
<fC07 i1="20" i2="X" l="ENG"><s0>Neurological disorder</s0>
<s5>45</s5>
</fC07>
<fC07 i1="20" i2="X" l="SPA"><s0>Trastorno neurológico</s0>
<s5>45</s5>
</fC07>
<fC07 i1="21" i2="X" l="FRE"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="21" i2="X" l="ENG"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="21" i2="X" l="SPA"><s0>Rodentia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="22" i2="X" l="FRE"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="22" i2="X" l="ENG"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="22" i2="X" l="SPA"><s0>Mammalia</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="23" i2="X" l="FRE"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="23" i2="X" l="ENG"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fC07 i1="23" i2="X" l="SPA"><s0>Vertebrata</s0>
<s2>NS</s2>
</fC07>
<fN21><s1>316</s1>
</fN21>
<fN44 i1="01"><s1>OTO</s1>
</fN44>
<fN82><s1>OTO</s1>
</fN82>
</pA>
</standard>
<server><NO>PASCAL 07-0480619 INIST</NO>
<ET>MIF-1 and its peptidomimetic analogs attenuate haloperidol-induced vacuous chewing movements and modulate apomorphine-induced rotational behavior in 6-hydroxydopamine-lesioned rats</ET>
<AU>CASTELLANO (Jessica M.); BATRYNCHUK (Jody); DOLBEARE (Kristine); VERMA (Vaneeta); MANN (Amandeep); SKOBLENICK (Kevin J.); JOHNSON (Rodney L.); MISHRA (Ram K.)</AU>
<AF>Department of Psychiatry and Behavioral Neurosciences, McMaster University, 1200 Main Street West/Hamilton, Ontario, L8N 3Z5/Canada (1 aut., 2 aut., 4 aut., 5 aut., 6 aut., 8 aut.); Department of Medicinal Chemistry, University of Minnesota/Minneapolis, MN 55455/Etats-Unis (3 aut., 7 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>Peptides : (New York, NY. 1980); ISSN 0196-9781; Coden PPTDD5; Etats-Unis; Da. 2007; Vol. 28; No. 10; Pp. 2009-2015; Bibl. 52 ref.</SO>
<LA>Anglais</LA>
<EA>Two melanocyte-stimulating hormone release inhibiting factor-1 (MIF-1) also known as L-prolyl-L-leucyl-glycinamide (PLG) peptidomimetic analogs, 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]-a mino] -3-(butyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (A) and 3(R)-[[[2(S)-pyrrolidinyl]carbonyl]amino]-3-(benzyl)-2-oxo-1-pyrrolidineacetamide trifluoroacetate (B), were evaluated for their ability to modulate dopaminergic activity by measuring apomorphine-induced rotations in 6-hydroxydopamine (6-OHDA)-lesioned rats, and haloperidol (HP)-induced vacuous chewing movements (VCMs) in rats; animal models of Parkinson's disease (PD) and human tardive dyskinesia (TD), respectively. In the 6-OHDA model, both analogs were found to potentiate the contralateral rotational behavior induced by apomorphine dose-dependently and with approximately the same potency. Furthermore, each analog was able to significantly attenuate HP-induced VCMs with almost equal efficacy. The potency and efficacy of these analogs were significantly greater than their parent compound, PLG. These results suggest that both analogs can modulate dopaminergic activity in vivo, likely by the same mechanisms recruited by PLG previously reported.</EA>
<CC>002A28; 002B17G; 002B17A01; 002B02B03</CC>
<FD>Analogue; Halopéridol; Mastication; Apomorphine; Comportement; Oxidopamine; Parkinson maladie; Animal; Contrôle moteur; Dyskinésie; Lésion; Dopamine; MSH; Libération; Rat</FD>
<FG>Psychotrope; Neuroleptique; Antagoniste dopamine; Butyrophénone dérivé; Récepteur dopaminergique D2; Agoniste; Récepteur dopaminergique D1; Stimulant dopaminergique; Récepteur adrénergique; Sympathomimétique; Catécholamine; Neurotransmetteur; Hormone hypophysaire; Encéphale pathologie; Extrapyramidal syndrome; Maladie dégénérative; Système nerveux central pathologie; Système nerveux pathologie; Mouvement involontaire; Trouble neurologique; Rodentia; Mammalia; Vertebrata</FG>
<ED>Analog; Haloperidol; Chewing; Behavior; Oxidopamine; Parkinson disease; Animal; Motor control; Dyskinesia; Lesion; Dopamine; Melanocyte stimulating hormone; Release; Rat</ED>
<EG>Psychotropic; Neuroleptic; Dopamine antagonist; Butyrophenone derivatives; D2 Dopamine receptor; Agonist; D1 Dopamine receptor; Dopamine agonist; Adrenergic receptor; Sympathomimetic; Catecholamine; Neurotransmitter; Pituitary hormone; Cerebral disorder; Extrapyramidal syndrome; Degenerative disease; Central nervous system disease; Nervous system diseases; Involuntary movement; Neurological disorder; Rodentia; Mammalia; Vertebrata</EG>
<SD>Análogo; Haloperidol; Masticación; Conducta; Oxidopamina; Parkinson enfermedad; Animal; Control motor; Disquinesia; Lesión; Dopamina; MSH; Liberación; Rata</SD>
<LO>INIST-19060.354000149842240110</LO>
<ID>07-0480619</ID>
</server>
</inist>
</record>
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