Dopamine D2 receptors selectively labeled by a benzamide neuroleptic: [3H]-YM-09151-2

Niznik, Hyman B.; Grigoriadis, Dimitri E.; Pri‐Bar, Ilan; Buchman, Ouri; Seeman, Philip

doi:10.1007/bf00496365

Cited by 107 publications

(36 citation statements)

References 34 publications

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“…However, the long-lasting nature of this effect cannot be explained by increased DA levels competing with [ 3 H]raclopride because DA levels are known to return to baseline at 2 h after amphetamine (Laruelle et al, 1997a (Niznik et al, 1985;Terai et al, 1989;Seeman et al, 1992). The "monomerdimer theory" has been evoked to account for these differences.…”

Section: Discussionmentioning

confidence: 99%

In Vivo Evidence for Dopamine-Mediated Internalization of D₂-Receptors after Amphetamine: Differential Findings with [³H]Raclopride versus [³H]Spiperone

Sun

Ginovart²,

Ko³

et al. 2003

Mol Pharmacol

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Competition with endogenous dopamine (DA) is usually invoked to explain changes in [11 C]raclopride binding observed after amphetamine administration in animals and humans. This account has recently been questioned because a number of inconsistencies have been reported that contradict it. In the present study, we investigated whether the decrease in [3 H]raclopride binding observed in the rat striatum after an amphetamine challenge reflects true competition with endogenous DA or agonist-mediated internalization of D 2 -receptors. We found that the amphetamine-induced decrease in The addition of Gpp(NH)p had no effect on B max , suggesting that these receptors were not just noncompetitively bound with dopamine at the cell-surface. Subcellular fractionation studies showed that amphetamine treatment led to a decrease in radioligand binding in the cell-surface fraction for both In vivo imaging techniques such as positron emission tomography (PET) and single-photon emission computed tomography (SPECT) have been applied to assess the endogenous levels of dopamine (DA) in both basic and clinical investigations. These techniques have been used to show that behavioral tasks, such as playing video games or writing, induce an increased release of striatal DA (Koepp et al., 1998;de la Fuente-Fernandez et al., 2001) and that patients with schizophrenia show an abnormally high release of DA when challenged with amphetamine (Laruelle et al., 1996;Breier et al., 1997). Although these techniques are being extensively used, PET and SPECT do not provide a direct measurement of endogenous DA levels. Changes in endogenous DA levels are inferred from changes in the binding of (Innis et al., 1992;Volkow et al., 1994;Laruelle et al., 1995;Smith et al., 1997), whereas the opposite effect is observed with drugs that decrease synaptic DA, such as reserpine and ␣-methyl-paratyrosine (Ginovart et al., 1997;Laruelle et al., 1997a

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Section: Discussionmentioning

confidence: 99%

In Vivo Evidence for Dopamine-Mediated Internalization of D₂-Receptors after Amphetamine: Differential Findings with [³H]Raclopride versus [³H]Spiperone

Sun

Ginovart²,

Ko³

et al. 2003

Mol Pharmacol

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“…M, standards, SDS and electrophoresis reagents were obtained from Bio-Rad; protease inhibitors from Sigma [6,12,13] …”

Section: Introduction 2 Materials and Methodsmentioning

confidence: 99%

Photoaffinity labelling of dopamine D₂ receptors by [³H]azidomethylspiperone

1986

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“…These studies use procedures that both address the abovementioned methodological concerns and, additionally, allow systematic comparison with the phenotype of congenic D 1 , D 2 , and D 3 receptor knockouts, which we have determined using these same procedures McNamara et al, 2002McNamara et al, , 2003. They contrast the effects of the selective D 2 -like receptor agonist RU 24213 (Euvrard et al, 1980;Clifford et al, 2000Clifford et al, , 2001McNamara et al, 2002McNamara et al, , 2003 with those of the selective D 2 -like receptor antagonist YM 09151-2 (Niznik et al, 1985;McNamara et al, 2003) to evaluate shifts in the topography of behavior mediated through D 2 -like receptors, consequent to the absence of DARPP-32.…”

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confidence: 99%

Ethologically Based Resolution of D₂-Like Dopamine Receptor Agonist-versus Antagonist-Induced Behavioral Topography in Dopamine- and Adenosine 3′,5′-Monophosphate-Regulated Phosphoprotein of 32 kDa “Knockout” Mutants Congenic on the C57BL/6 Genetic Background

Nally

Kinsella²,

Tighe³

et al. 2004

J Pharmacol Exp Ther

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Given the critical role of dopamine-and adenosine 3Ј,5Ј-monophosphate-regulated phosphoprotein of 32 kDa in the regulation of dopaminergic function, DARPP-32-null mutant mice congenic on the inbred C57BL/6 strain for 10 generations were examined phenotypically for their ethogram of responsivity to the selective D 2 -like receptor agonist RU 24213 (N-npropyl-N-phenylethyl-p-3-hydroxyphenylethylamine) and the selective D 2 -like receptor antagonist YM 09151-2 (cis-N-[1-benzyl-2-methyl-pyrrolidin-3-yl]-5-chloro-2-methoxy-4-methylaminobenzamide), using procedures that resolve all topographies of behavior in the natural repertoire. After vehicle challenge, levels of sniffing and rearing seated were reduced in DARPP-32 mutants; the injection procedure seems to constitute a "stressor" that reveals phenotypic effects of DARPP-32 deletion not apparent under natural conditions. Topographical effects of 0.3 to 10.0 mg/kg RU 24213, primarily induction of sniffing and ponderous locomotion with accompanying reductions in rearing, grooming, sifting and chewing, were not altered to any material extent in DARPP-32-null mice. However, topographical effects of 0.005 to 0.625 mg/kg YM 09151-2, namely, reduction in sniffing, locomotion, rearing, grooming, and chewing but not sifting, were essentially absent in DARPP-32 mutants. Thus, the D 2 -like receptor agonist-mediated ethogram was essentially conserved, whereas major elements of the corresponding D 2 -like receptor antagonist-mediated ethogram were essentially absent in DARPP-32-null mice. This suggests some relationship between 1) extent of tonic dopaminergic activation of DARPP-32 mechanisms and 2) compensatory mechanisms consequent to the developmental absence of DARPP-32, which may emerge to act differentially on individual elements of the DARPP-32 system. Critically, the present data indicate that phenotypic effects of a given gene deletion using an agonist acting on the system disrupted cannot be generalized to a corresponding antagonist, and vice versa. subtypes in the regulation of mammalian behavior remains uncertain because of delay in the identification of a full range of selective agonists and antagonists by medicinal chemistry relative to the rate of identification of these receptor subtypes by molecular biology (Waddington et al., 1995;Di Chiara, 2002;Sidhu et al., 2003). The construction of mutants with targeted gene deletion ("knockout") of each individual dopamine receptor subtype has provided an important approach to addressing this issue (Sibley, 1999;Waddington et al., 2001). However, elucidation of the

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Dopamine D2 receptors selectively labeled by a benzamide neuroleptic: [3H]-YM-09151-2

Cited by 107 publications

References 34 publications

In Vivo Evidence for Dopamine-Mediated Internalization of D₂-Receptors after Amphetamine: Differential Findings with [³H]Raclopride versus [³H]Spiperone

In Vivo Evidence for Dopamine-Mediated Internalization of D₂-Receptors after Amphetamine: Differential Findings with [³H]Raclopride versus [³H]Spiperone

Photoaffinity labelling of dopamine D₂ receptors by [³H]azidomethylspiperone

Ethologically Based Resolution of D₂-Like Dopamine Receptor Agonist-versus Antagonist-Induced Behavioral Topography in Dopamine- and Adenosine 3′,5′-Monophosphate-Regulated Phosphoprotein of 32 kDa “Knockout” Mutants Congenic on the C57BL/6 Genetic Background

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Dopamine D2 receptors selectively labeled by a benzamide neuroleptic: [3H]-YM-09151-2

Cited by 107 publications

References 34 publications

In Vivo Evidence for Dopamine-Mediated Internalization of D2-Receptors after Amphetamine: Differential Findings with [3H]Raclopride versus [3H]Spiperone

In Vivo Evidence for Dopamine-Mediated Internalization of D2-Receptors after Amphetamine: Differential Findings with [3H]Raclopride versus [3H]Spiperone

Photoaffinity labelling of dopamine D2 receptors by [3H]azidomethylspiperone

Ethologically Based Resolution of D2-Like Dopamine Receptor Agonist-versus Antagonist-Induced Behavioral Topography in Dopamine- and Adenosine 3′,5′-Monophosphate-Regulated Phosphoprotein of 32 kDa “Knockout” Mutants Congenic on the C57BL/6 Genetic Background

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In Vivo Evidence for Dopamine-Mediated Internalization of D₂-Receptors after Amphetamine: Differential Findings with [³H]Raclopride versus [³H]Spiperone

In Vivo Evidence for Dopamine-Mediated Internalization of D₂-Receptors after Amphetamine: Differential Findings with [³H]Raclopride versus [³H]Spiperone

Photoaffinity labelling of dopamine D₂ receptors by [³H]azidomethylspiperone

Ethologically Based Resolution of D₂-Like Dopamine Receptor Agonist-versus Antagonist-Induced Behavioral Topography in Dopamine- and Adenosine 3′,5′-Monophosphate-Regulated Phosphoprotein of 32 kDa “Knockout” Mutants Congenic on the C57BL/6 Genetic Background