Effects of the D3 preferring dopamine agonist pramipexole on sleep and waking, locomotor activity and striatal dopamine release in rats

Lagos, Patricia; Scorza, Cecilia; Monti, Jaime M.; Jantos, Héctor; Reyes‐Parada, Miguel; Silveira, Ricardo dos Reis; Ponzoni, Ana

doi:10.1016/s0924-977x(97)00054-0

Cited by 62 publications

(32 citation statements)

References 18 publications

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“…In our current studies, the activity of PRAM in the forced swim test was not due to a generalized increase in locomotor activity, since PRAM administration, at doses that were efficacious in the forced swim test, produced decreases, rather than increases in locomotor activity. Several previous studies have reported dose-dependent changes in locomotor activity after acute or chronic PRAM administration in both mice and rats (Mierau and Schingnitz 1992;Svensson et al 1994;Maj et al 1997a,b;Lagos et al 1998;Maj and Rogoz 1999), with hypoactivity generally seen at lower doses and hyperactivity sometimes observed at higher doses. Our current studies using unhabituated CD-1 mice demonstrate a dose-dependent reduction in locomotor activity, which was evident within the first hour after drug administration.…”

Section: Discussionmentioning

confidence: 93%

The activity of pramipexole in the mouse forced swim test is mediated by D2 rather than D3 receptors

Siuciak

Fujiwara

2004

Psychopharmacology

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Section: Discussionmentioning

confidence: 93%

The activity of pramipexole in the mouse forced swim test is mediated by D2 rather than D3 receptors

Siuciak

Fujiwara

2004

Psychopharmacology

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“…(Friedman, 1995). D 3 receptor agonists have also been shown to decrease locomotor activity (Lagos et al, 1998). This suggests that sumanirole's unique selectivity may confer beneficial effects in the treatment of Parkinson's disease.…”

Section: Discussionmentioning

confidence: 99%

Sumanirole, a Highly Dopamine D₂-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson's Disease

McCall

Lookingland

Bédard

et al. 2005

J Pharmacol Exp Ther

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The purpose of this study is to demonstrate that sumanirole is a novel dopamine receptor agonist with high in vitro and in vivo selectivity for the D 2 receptor subtype. Sumanirole, (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Z)-2-butenedioate (1:1), is unique; it has greater than 200-fold selectivity for the D 2 receptor subtype versus the other dopamine receptor subtypes in radioligand binding assays. In cell-based assays, sumanirole is a fully efficacious agonist, with EC 50 values between 17 and 75 nM. In animals, sumanirole elicits many physiological responses attributed to D 2 -like receptor function. In rats, sumanirole is a full agonist for elevation of striatal acetylcholine levels (ED 50 ϭ 12.1 mol/kg i.p.). Sumanirole s.c. dose dependently decreased plasma prolactin levels and depressed dopamine neuron firing rates in the substantia nigra pars compacta with an ED 50 of 2.3 mol/kg i.v. This high selectivity for D 2 receptors translates into excellent locomotor stimulant activity in animal models of Parkinson's disease. In reserpinized, ␣-methyl-para-tyrosine-treated rats, sumanirole caused a significant and sustained increase in horizontal activity at doses Ն12.5 mol/kg s.c. In unilateral 6-hydroxydopamine-lesioned rats, sumanirole caused profound, sustained rotational behavior and was substantially more efficacious than any other agonist tested. Sumanirole-stimulated rotational behavior was blocked by the dopamine receptor antagonist haloperidol. Sumanirole dose dependently improved disability scores and locomotor activities of two of three 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned monkeys. In summary, sumanirole is the first published selective D 2 receptor agonist. The compound has activity in animal models of dopamine hypofunction and has a high level of efficacy in animal models of Parkinson's disease.Parkinson's disease results from degeneration of the dopaminergic cells in the substantia nigra and is characterized by bradykinesia, tremors, and muscular rigidity. Several dopamine receptor agonists have been used as antiparkinsonian therapy, including bromocriptine, cabergoline, pergolide, pramipexole, and ropinirole (Hagan et al., 1997). Pramipexole, cabergoline, and ropinirole are effective as monotherapy in early stage Parkinson's disease and their use significantly delays the initiation of L-dopa therapy (Inzelberg et al., 2003;Bracco et al., 2004). Dopamine agonists are also used as adjuncts to L-dopa. The combined treatment enables lower doses of L-dopa, which decreases the incidence of response fluctuations and dyskinesias. However, currently available dopaminergic therapy, including agonists and L-dopa therapy, can elicit side effects, including psychiatric complications and somnolence (Lieberman, 1995). Thus, there is a need for new compounds with fewer side effects (Hobson et al., 2002;Etminan et al., 2003).There are at least five subtypes of dopamine receptors, grouped into two subfamilies, D 1 -like and D 2 -like, based on pharmacological...

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“…Moreover, systemic administration of D1 receptor agonists and antagonists increase and decrease, respectively, time spent awake (Monti et al, 1990;Trampus et al, 1991). D2 receptor agonists exert more complex effects, likely reflecting both presynaptic and postsynaptic functions of this receptor family (Monti et al, 1989;Python et al, 1996;Lagos et al, 1998;Olive et al, 1998). When administered centrally (i.c.v.)…”

Section: Wake-promoting Actions Of Damentioning

confidence: 99%

Neural Substrates of Psychostimulant-Induced Arousal

Berridge

2006

Neuropsychopharmacol

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Extensive research has provided substantial insight into the neurobiological mechanisms underlying the reinforcing, locomotor-activating and stereotypy-inducing actions of psychostimulants. The diverse behavioral effects of these drugs are superimposed on potent arousalenhancing actions. Psychostimulant-induced arousal is a prominent contributing factor to the widespread use and abuse of these drugs. Moreover, enhanced arousal may be a critical component of the reinforcing and other behavioral actions of these drugs. Although long overlooked, recent work begins to identify the neural mechanisms involved in psychostimulant-induced arousal. For example, microdialysis studies demonstrate a close relationship between amphetamine-induced waking/arousal and amphetamine-induced increases in norepinephrine and dopamine efflux. Additionally, it is now clear that both norepinephrine and dopamine exert robust wakepromoting actions. The wake-promoting effects of norepinephrine involve synergistic actions of a 1 -and b-receptors, whereas dopamineinduced waking involves both D1 and D2 receptors. Finally, additional studies have identified subcortical regions involved in the wakepromoting actions of both norepinephrine and amphetamine. These regions include, but may not be limited to, the medial septal area, the medial preoptic area, and the lateral hypothalamus. Combined, these and other observations indicate a prominent involvement of both norepinephrine and dopamine in stimulant-induced arousal via actions within a network of subcortical regions. Although it is clear that both norepinephrine and dopamine contribute to psychostimulant-induced arousal, the degree to which each transmitter system is necessary for the expression of stimulant-induced arousal remains to be fully elucidated.

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Effects of the D3 preferring dopamine agonist pramipexole on sleep and waking, locomotor activity and striatal dopamine release in rats

Cited by 62 publications

References 18 publications

The activity of pramipexole in the mouse forced swim test is mediated by D2 rather than D3 receptors

The activity of pramipexole in the mouse forced swim test is mediated by D2 rather than D3 receptors

Sumanirole, a Highly Dopamine D₂-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson's Disease

Neural Substrates of Psychostimulant-Induced Arousal

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Effects of the D3 preferring dopamine agonist pramipexole on sleep and waking, locomotor activity and striatal dopamine release in rats

Cited by 62 publications

References 18 publications

The activity of pramipexole in the mouse forced swim test is mediated by D2 rather than D3 receptors

The activity of pramipexole in the mouse forced swim test is mediated by D2 rather than D3 receptors

Sumanirole, a Highly Dopamine D2-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson's Disease

Neural Substrates of Psychostimulant-Induced Arousal

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Sumanirole, a Highly Dopamine D₂-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson's Disease