Biochemical and pharmacological studies on pramipexole, a potent and selective dopamine D2 receptor agonist

Mierau, Joachim; Schingnitz, G.

doi:10.1016/0014-2999(92)90024-x

Cited by 123 publications

(47 citation statements)

References 27 publications

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“…We found that SKF 83822 was able to induce intense, dose dependent, contralateral rotation in rats with unilateral 6-OHDA lesions which could be virtually abolished by pretreatment with the selective D1 antagonist SCH-23390. In contrast, previous studies have found that SCH-23390, even at substantially higher doses than those used here, only partially attenuates D2 agonist induced rotation (Arnt and Hyttel, 1984;Mierau and Schingnitz, 1992). Treatment with SKF 83822 also induced intense expression of the immediate early genes c-fos, Fra-2 and Zif/268 and of the activity regulated cytoskeletal protein Arc in the deinnervated striatum and these effects could again be blocked by pretreatment with SCH-23390, confirming that they were dependent on stimulation of D1-like receptors.…”

Section: Discussioncontrasting

confidence: 99%

Rotation and immediate-early gene expression in rats treated with the atypical D1 dopamine agonist SKF 83822

Wirtshafter

2007

Pharmacology Biochemistry and Behavior

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Classical agonists of the dopamine D1 receptor activate both adenylyl cyclase and phospholipase C (PLC) signaling pathways. As a result, the extent to which these two pathways are essentially involved in various effects produced by D1 receptor agonists is currently uncertain. In the present report we examined the effects of SKF 83822, a dopamine D1 agonist which has been reported to activate adenylyl cyclase, but not PLC, on behavior and immediate early gene (IEG) expression in rats with unilateral 6-hydroxydopamine lesions. SKF 83822 (25-100 ug/kg) induced dose dependent contralateral rotation in these subjects, and, additionally, stimulated strong expression of the IEG products c-Fos, Fra2, Zif/268 and Arc in the deinnervated striatum. All of these effects could be antagonized by pretreatment with the selective D1 dopamine antagonist SCH 23390 (0.5 mg/kg). Although PLC may be involved in many effects mediated through dopamine D1 receptors, these results suggest that direct activation of PLC is not necessary for the induction of either rotation or IEG expression in dopamine depleted rats.

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Section: Discussioncontrasting

confidence: 99%

Rotation and immediate-early gene expression in rats treated with the atypical D1 dopamine agonist SKF 83822

Wirtshafter

2007

Pharmacology Biochemistry and Behavior

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“…In fact, we observed that the dose-response curve for OLDA was bell-shaped, as are those reported for a number of direct and indirect dopaminergic agents (15)(16). Moreover, it is well documented that hyperactivity induced by both direct and indirect DA agonists is blocked by haloperidol (17)(18)(19)(20), a preferential D 2 receptor antagonist (21)(22). In the present study, haloperidol prevented, in a dose-dependent manner, the OLDA-induced hyperlocomotion, not altering basal locomotor activity in well-habituated animals.…”

Section: Discussionsupporting

confidence: 81%

N-Oleoyl-Dopamine Increases Locomotor Activity in the Rat

Przegaliński

Filip²,

Zając

et al. 2006

Int J Immunopathol Pharmacol

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N-oleoyl-dopamine (OLDA), a condensation product of oleic acid and dopamine (DA), is a bioactive lipid whose biological functions are not yet fully explored. The compound crosses the blood-brain barrier and might be considered as a carrier of DA into the brain. In this study we sought to determine whether OLDA would influence locomotor behavior and whether the central DA system would be involved in such influence. We addressed this issue by investigating horizontal locomotor activity in male Wistar rats after intraperitoneal administration of OLDA, 5-20 mg/kg, before and after pretreatment with haloperidol, a D z receptor antagonist. We found that OLDA caused a prompt stimulation of locomotor activity, with a bell-shaped dose-response. The maximum stimulatory effect was observed after 10 mg/kg of OLDA where the mean distance traveled by rats during a 2-hour test increased to 1213 ±196(SE) em from the 403 ±89 em in the vehicle-treated rats (P<0.05). This effect was dose-dependently antagonized by haloperidol (0.1-0.2 mg/kg). The results support the hypothesis that the OLDA-induced hyperlocomotion was mediated by the stimulation of DA systems. Using in vitro assays, we further demonstrated that OLDA is a stable compound that resists hydrolysis over a 2-hour period and thus the integral OLDA compound exerted DA-Iike effects. We conclude that OLDA is a potential brain modifier of motor behavior, the biological consequences of which remain to be explored.

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“…However, the aminobenzothiazole compound pramipexole (Fig. 1), a potent dopamine autoreceptor agonist that stimulates members of the postsynaptic D 2 receptor family (D 2 , D 3 , and D 4 ), improving the symptoms of Parkinson's disease (Mierau and Schingnitz, 1992;Mierau et al, 1995;Domino et al, 1997), is being introduced for the treatment of both early-and advanced-stage Parkinson's disease. The absolute bioavailability of pramipexole after oral administration in humans is over 90%.…”

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confidence: 99%

TRANSPORT OF THE DOPAMINE D₂ AGONIST PRAMIPEXOLE BY RAT ORGANIC CATION TRANSPORTERS OCT1 AND OCT2 IN KIDNEY

Ishiguro¹,

Saito²,

Yokoyama³

et al. 2005

Drug Metab Dispos

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Biochemical and pharmacological studies on pramipexole, a potent and selective dopamine D2 receptor agonist

Cited by 123 publications

References 27 publications

Rotation and immediate-early gene expression in rats treated with the atypical D1 dopamine agonist SKF 83822

Rotation and immediate-early gene expression in rats treated with the atypical D1 dopamine agonist SKF 83822

N-Oleoyl-Dopamine Increases Locomotor Activity in the Rat

TRANSPORT OF THE DOPAMINE D₂ AGONIST PRAMIPEXOLE BY RAT ORGANIC CATION TRANSPORTERS OCT1 AND OCT2 IN KIDNEY

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Biochemical and pharmacological studies on pramipexole, a potent and selective dopamine D2 receptor agonist

Cited by 123 publications

References 27 publications

Rotation and immediate-early gene expression in rats treated with the atypical D1 dopamine agonist SKF 83822

Rotation and immediate-early gene expression in rats treated with the atypical D1 dopamine agonist SKF 83822

N-Oleoyl-Dopamine Increases Locomotor Activity in the Rat

TRANSPORT OF THE DOPAMINE D2 AGONIST PRAMIPEXOLE BY RAT ORGANIC CATION TRANSPORTERS OCT1 AND OCT2 IN KIDNEY

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TRANSPORT OF THE DOPAMINE D₂ AGONIST PRAMIPEXOLE BY RAT ORGANIC CATION TRANSPORTERS OCT1 AND OCT2 IN KIDNEY