The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Sadako Kuno - One of the best experts on this subject based on the ideXlab platform.
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combination treatment of the partial d2 agonist Terguride with the d1 agonist skf 82958 in 1 methyl 4 phenyl 1 2 3 6 tetrahydropyridine lesioned parkinsonian cynomolgus monkeys
Journal of Pharmacology and Experimental Therapeutics, 1995Co-Authors: T. Akai, M. Yamaguchi, Eiji Mizuta, M Ozawa, Sadako KunoAbstract:The optimal combination of a dopamine D2 agonist and a D1 agonist was evaluated for symptomatic treatment of Parkinson's disease. Behavioral effects of combination treatment of the full D2 agonist quinpirole or the partial D2 agonist Terguride with the full D1 agonist SKF 82958 [(I) 6-Chloro-7, 8-dihydroxy-3-allyl-1-phenyl-2, 3, 4, 5-tetra-hydro-1H-3-benzazepine] were investigated in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys with attention to the induction of hyperactivity such as irritability, excitability and aggressiveness and of dyskinesias such as licking of paws, chewing and biting. Both quinpirole and SKF 82958 alone improved the parkinsonism with a slight induction of the hyperactivity and dyskinesias. Terguride also improved the parkinsonism but did not induce the hyperactivity and dyskinesias. Combination treatment of quinpirole with SKF 82958 not only showed a tendency to augment the antiparkinsonian effects but also induced the marked hyperactivity and dyskinesias. On the other hand, combination treatment of Terguride with SKF 82958 also augmented the antiparkinsonian effects but did not induce any hyperactivity and dyskinesias. These findings suggest that combination therapy with a partial D2 agonist and a full D1 agonist or monotherapy with a dopamine agonist that has both partial D2 and full D1 agonist properties might be beneficial for treating motor dysfunction in Parkinson's disease without inducing dopaminergic side effects.
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effects of Terguride a partial d2 agonist on mptp lesioned parkinsonian cynomolgus monkeys
Annals of Neurology, 1993Co-Authors: Tetsuo Akai, Motonori Yamaguchi, Eiji Mizuta, Sadako KunoAbstract:Behavioral effects of Terguride, a partial dopamine D2 agonist, on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys were compared with those of the dopamine agonist apomorphine and the dopamine antagonist haloperidol. Terguride alone ameliorated the parkinsonism without inducing any sign of excitability, irritability, or aggressiveness (hyperactivity). Apomorphine alone also ameliorated the parkinsonism but induced marked hyperactivity. Haloperidol alone caused worsening of the parkinsonism, inducing transient eyelid closure. In combination with apomorphine, Terguride suppressed the hyperactivity induced by apomorphine without reducing its antiparkinsonian effects. Pretreatment with haloperidol suppressed both the antiparkinsonian effects and the hyperactivity induced by apomorphine. Terguride thus exhibits both antiparkinsonian and antihyperactivity effects in a monkey model of Parkinson's disease, suggesting that Terguride might be beneficial for treating motor dysfunction and dopaminergic psychosis in advanced Parkinson's disease.
T. Akai - One of the best experts on this subject based on the ideXlab platform.
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combination treatment of the partial d2 agonist Terguride with the d1 agonist skf 82958 in 1 methyl 4 phenyl 1 2 3 6 tetrahydropyridine lesioned parkinsonian cynomolgus monkeys
Journal of Pharmacology and Experimental Therapeutics, 1995Co-Authors: T. Akai, M. Yamaguchi, Eiji Mizuta, M Ozawa, Sadako KunoAbstract:The optimal combination of a dopamine D2 agonist and a D1 agonist was evaluated for symptomatic treatment of Parkinson's disease. Behavioral effects of combination treatment of the full D2 agonist quinpirole or the partial D2 agonist Terguride with the full D1 agonist SKF 82958 [(I) 6-Chloro-7, 8-dihydroxy-3-allyl-1-phenyl-2, 3, 4, 5-tetra-hydro-1H-3-benzazepine] were investigated in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys with attention to the induction of hyperactivity such as irritability, excitability and aggressiveness and of dyskinesias such as licking of paws, chewing and biting. Both quinpirole and SKF 82958 alone improved the parkinsonism with a slight induction of the hyperactivity and dyskinesias. Terguride also improved the parkinsonism but did not induce the hyperactivity and dyskinesias. Combination treatment of quinpirole with SKF 82958 not only showed a tendency to augment the antiparkinsonian effects but also induced the marked hyperactivity and dyskinesias. On the other hand, combination treatment of Terguride with SKF 82958 also augmented the antiparkinsonian effects but did not induce any hyperactivity and dyskinesias. These findings suggest that combination therapy with a partial D2 agonist and a full D1 agonist or monotherapy with a dopamine agonist that has both partial D2 and full D1 agonist properties might be beneficial for treating motor dysfunction in Parkinson's disease without inducing dopaminergic side effects.
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Terguride, a dopamine D(2) partial agonist, as a discriminative stimulus in rats.
Behavioural pharmacology, 1991Co-Authors: M. Yamaguchi, K. Kimura-iwasaki, T. Akai, Y. Nakada, H. NakagawaAbstract:Drug discrimination training with Terguride, a 9, 10-transdihydrogenated derivative of lisuride, was carried out using a two-lever food-reinforced procedure (FR 10) in rats, to investigate its influence on central dopaminergic (DA) and serotonergic (5-HT) functions. The Terguride (0.05mg/kg, i.p.) discrimination was established within 64 +/- 5 training sessions (mean +/- S.E.) and was stably maintained thereafter. Higher doses of Terguride could not be used for discriminative training due to response disruption. In generalization tests with Terguride, drug-appropriate responding increased dose-dependently and reached levels of 45 and 99% at 0.01 and 0.05mg/kg i.p. The D(2) agonist lisuride at low doses and the DA autoreceptor agonist (-)-3-PPP substituted for Terguride. The DA agonist apomorphine and the 5-HT agonist 5-MeO-DMT produced dose-dependent but incomplete substitution. The D(1) agonist SKF38393, the DA antagonist haloperidol, the D(2) antagonist sulpiride, the D(1) antagonist SCH23390, the 5-HT(1A) agonist 8-OH-DPAT, the 5-HT(1B) agonist m-CPP and the 5-HT(2) agonist DOI were not generalized. In antagonism tests, sulpride completely blocked the Terguride-appropriate response, but SCH23390 and the 5-HT antagonist methysergide did not. These results indicate that discriminative stimulus properties of Terguride in rats are mediated primarily by activation of receptors with characteristics similar to those of presynaptic D(2) autoreceptors.
Eiji Mizuta - One of the best experts on this subject based on the ideXlab platform.
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combination treatment of the partial d2 agonist Terguride with the d1 agonist skf 82958 in 1 methyl 4 phenyl 1 2 3 6 tetrahydropyridine lesioned parkinsonian cynomolgus monkeys
Journal of Pharmacology and Experimental Therapeutics, 1995Co-Authors: T. Akai, M. Yamaguchi, Eiji Mizuta, M Ozawa, Sadako KunoAbstract:The optimal combination of a dopamine D2 agonist and a D1 agonist was evaluated for symptomatic treatment of Parkinson's disease. Behavioral effects of combination treatment of the full D2 agonist quinpirole or the partial D2 agonist Terguride with the full D1 agonist SKF 82958 [(I) 6-Chloro-7, 8-dihydroxy-3-allyl-1-phenyl-2, 3, 4, 5-tetra-hydro-1H-3-benzazepine] were investigated in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys with attention to the induction of hyperactivity such as irritability, excitability and aggressiveness and of dyskinesias such as licking of paws, chewing and biting. Both quinpirole and SKF 82958 alone improved the parkinsonism with a slight induction of the hyperactivity and dyskinesias. Terguride also improved the parkinsonism but did not induce the hyperactivity and dyskinesias. Combination treatment of quinpirole with SKF 82958 not only showed a tendency to augment the antiparkinsonian effects but also induced the marked hyperactivity and dyskinesias. On the other hand, combination treatment of Terguride with SKF 82958 also augmented the antiparkinsonian effects but did not induce any hyperactivity and dyskinesias. These findings suggest that combination therapy with a partial D2 agonist and a full D1 agonist or monotherapy with a dopamine agonist that has both partial D2 and full D1 agonist properties might be beneficial for treating motor dysfunction in Parkinson's disease without inducing dopaminergic side effects.
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effects of Terguride a partial d2 agonist on mptp lesioned parkinsonian cynomolgus monkeys
Annals of Neurology, 1993Co-Authors: Tetsuo Akai, Motonori Yamaguchi, Eiji Mizuta, Sadako KunoAbstract:Behavioral effects of Terguride, a partial dopamine D2 agonist, on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys were compared with those of the dopamine agonist apomorphine and the dopamine antagonist haloperidol. Terguride alone ameliorated the parkinsonism without inducing any sign of excitability, irritability, or aggressiveness (hyperactivity). Apomorphine alone also ameliorated the parkinsonism but induced marked hyperactivity. Haloperidol alone caused worsening of the parkinsonism, inducing transient eyelid closure. In combination with apomorphine, Terguride suppressed the hyperactivity induced by apomorphine without reducing its antiparkinsonian effects. Pretreatment with haloperidol suppressed both the antiparkinsonian effects and the hyperactivity induced by apomorphine. Terguride thus exhibits both antiparkinsonian and antihyperactivity effects in a monkey model of Parkinson's disease, suggesting that Terguride might be beneficial for treating motor dysfunction and dopaminergic psychosis in advanced Parkinson's disease.
Roger D Spealman - One of the best experts on this subject based on the ideXlab platform.
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Suppression of cocaine- and food-maintained behavior by the D2-like receptor partial agonist Terguride in squirrel monkeys.
Psychopharmacology, 2003Co-Authors: Donna M. Platt, Joshua S. Rodefer, James K Rowlett, Roger D SpealmanAbstract:Rationale The D2-like receptor partial agonist Terguride has a profile of behavioral effects in rats that suggests potential benefit as a pharmacotherapy for cocaine addiction.
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discriminative stimulus effects of cocaine in squirrel monkeys lack of antagonism by the dopamine d2 partial agonists Terguride sdz 208 911 and sdz 208 912
Pharmacology Biochemistry and Behavior, 1995Co-Authors: Roger D SpealmanAbstract:Abstract The effects of cocaine alone and after pretreatment with the dopamine D 2 partial agonists Terguride, SDZ 208-911, and SDZ 202-912 were determined in squirrel monkeys trained to discriminate cocaine from saline using a two-lever drug discrimination procedure. When tested alone, cocaine engendered dose-related increases in the percentage of responses on the cocaineassociated lever, reaching virtually exclusive cocaine-appropriate responding after a dose of 1.0 mg/kg. Pretreatment with Terguride (0.003–0.03 mg/kg), SDZ 208-911 (0.001–0.01), and SDZ 208-912 (0.003–0.018 mg/kg) did not consistently alter the discriminative stimulus effects of cocaine. Although some doses of each D 2 partial agonist either increased (notably SDZ 208-911) or decreased (notably SDZ 208-912) the level of cocaine-appropriate responding engendered by low to intermediate doses of cocaine, none of the drugs reduced the percentage of cocaine-appropriate responses engendered by 1.0 mg/kg cocaine. The results do not support the view that Terguride, SDZ 208-911, or SDZ 208-912 would serve as functional antagonists of the subjective effects of cocaine.
M. Yamaguchi - One of the best experts on this subject based on the ideXlab platform.
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combination treatment of the partial d2 agonist Terguride with the d1 agonist skf 82958 in 1 methyl 4 phenyl 1 2 3 6 tetrahydropyridine lesioned parkinsonian cynomolgus monkeys
Journal of Pharmacology and Experimental Therapeutics, 1995Co-Authors: T. Akai, M. Yamaguchi, Eiji Mizuta, M Ozawa, Sadako KunoAbstract:The optimal combination of a dopamine D2 agonist and a D1 agonist was evaluated for symptomatic treatment of Parkinson's disease. Behavioral effects of combination treatment of the full D2 agonist quinpirole or the partial D2 agonist Terguride with the full D1 agonist SKF 82958 [(I) 6-Chloro-7, 8-dihydroxy-3-allyl-1-phenyl-2, 3, 4, 5-tetra-hydro-1H-3-benzazepine] were investigated in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys with attention to the induction of hyperactivity such as irritability, excitability and aggressiveness and of dyskinesias such as licking of paws, chewing and biting. Both quinpirole and SKF 82958 alone improved the parkinsonism with a slight induction of the hyperactivity and dyskinesias. Terguride also improved the parkinsonism but did not induce the hyperactivity and dyskinesias. Combination treatment of quinpirole with SKF 82958 not only showed a tendency to augment the antiparkinsonian effects but also induced the marked hyperactivity and dyskinesias. On the other hand, combination treatment of Terguride with SKF 82958 also augmented the antiparkinsonian effects but did not induce any hyperactivity and dyskinesias. These findings suggest that combination therapy with a partial D2 agonist and a full D1 agonist or monotherapy with a dopamine agonist that has both partial D2 and full D1 agonist properties might be beneficial for treating motor dysfunction in Parkinson's disease without inducing dopaminergic side effects.
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Terguride, a dopamine D(2) partial agonist, as a discriminative stimulus in rats.
Behavioural pharmacology, 1991Co-Authors: M. Yamaguchi, K. Kimura-iwasaki, T. Akai, Y. Nakada, H. NakagawaAbstract:Drug discrimination training with Terguride, a 9, 10-transdihydrogenated derivative of lisuride, was carried out using a two-lever food-reinforced procedure (FR 10) in rats, to investigate its influence on central dopaminergic (DA) and serotonergic (5-HT) functions. The Terguride (0.05mg/kg, i.p.) discrimination was established within 64 +/- 5 training sessions (mean +/- S.E.) and was stably maintained thereafter. Higher doses of Terguride could not be used for discriminative training due to response disruption. In generalization tests with Terguride, drug-appropriate responding increased dose-dependently and reached levels of 45 and 99% at 0.01 and 0.05mg/kg i.p. The D(2) agonist lisuride at low doses and the DA autoreceptor agonist (-)-3-PPP substituted for Terguride. The DA agonist apomorphine and the 5-HT agonist 5-MeO-DMT produced dose-dependent but incomplete substitution. The D(1) agonist SKF38393, the DA antagonist haloperidol, the D(2) antagonist sulpiride, the D(1) antagonist SCH23390, the 5-HT(1A) agonist 8-OH-DPAT, the 5-HT(1B) agonist m-CPP and the 5-HT(2) agonist DOI were not generalized. In antagonism tests, sulpride completely blocked the Terguride-appropriate response, but SCH23390 and the 5-HT antagonist methysergide did not. These results indicate that discriminative stimulus properties of Terguride in rats are mediated primarily by activation of receptors with characteristics similar to those of presynaptic D(2) autoreceptors.
