Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. II. Agonist and Antagonist Properties at Subtypes of Dopamine D2-Like Receptor and α1/α2-Adrenoceptor

@article{NewmanTancredi2002DifferentialAO,
  title={Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. II. Agonist and Antagonist Properties at Subtypes of Dopamine D2-Like Receptor and $\alpha$1/$\alpha$2-Adrenoceptor},
  author={Adrian Newman-Tancredi and Didier Cussac and Valérie Audinot and Jean Paul Nicolas and Fr{\'e}d{\'e}ric De Ceuninck and Jean A. Boutin and Mark J Millan},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2002},
  volume={303},
  pages={805 - 814}
}
The accompanying multivariate analysis of the binding profiles of antiparkinson agents revealed contrasting patterns of affinities at diverse classes of monoaminergic receptor. Herein, we characterized efficacies at human (h)D2SHORT(S), hD2LONG(L), hD3, and hD4.4receptors and at hα2A-, hα2B-, hα2C-, and hα1A-adrenoceptors (ARs). As determined by guanosine 5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding, no ligand displayed “full” efficacy relative to dopamine (100%) at all “D2-like” sites… 
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Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. III. Agonist and Antagonist Properties at Serotonin, 5-HT1 and 5-HT2, Receptor Subtypes
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Antiparkinson agents display markedly different patterns of agonist and antagonist properties at multiple 5-HT receptor subtypes, although all show modest (agonist) activity at5-HT1A sites, and their contrasting actions at 5-ht2A and 5- HT2C sites may be of particular significance to their functional profiles in vivo.
Differential Actions of Antiparkinson Agents at Multiple Classes of Monoaminergic Receptor. I. A Multivariate Analysis of the Binding Profiles of 14 Drugs at 21 Native and Cloned Human Receptor Subtypes
TLDR
An innovative multivariate analysis revealed marked heterogeneity in binding profiles of antiparkinson agents at diverse receptors implicated in the etiology and/or treatment of Parkinson's disease.
Pharmacological Profile of 2-Bromoterguride at Human Dopamine D2, Porcine Serotonin 5-Hydroxytryptamine 2A, and α2C-Adrenergic Receptors, and Its Antipsychotic-Like Effects in Rats
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2-bromoterguride may be a strong candidate for the treatment of schizophrenia with a lower risk to induce EPS because of its in vitro and in vivo properties.
Discriminative stimulus properties of S32504, a novel D3/D2 receptor agonist and antiparkinson agent, in rats: attenuation by the antipsychotics, aripiprazole, bifeprunox, N-desmethylclozapine, and by selective antagonists at dopamine D2 but not D3 receptors
TLDR
The antiparkinson agent, S32504, displays DS properties principally mediated by high-efficacy activation of D2 receptors Antipsychotics known to act as partial agonists at D2/D3 receptors attenuate DS properties of S32 504, actions reflecting their low efficacy at these sites.
Differential induction of adenylyl cyclase supersensitivity by antiparkinson drugs acting as agonists at dopamine D1/D2/D3 receptors vs D2/D3 receptors only: Parallel observations from co-transfected human and native cerebral receptors
TLDR
AC supersensitivity is elicited by the sustained exposure of cloned human and native mouse populations of dopaminergic receptors, to D(2/D(3) but not D(1)/D(2)/D (3) agonists, which may be related to the exacerbation of gambling in Parkinson's disease that is provoked by antiparkinson agents acting as selective D( 2)/D3) receptor agonists.
From the cell to the clinic: a comparative review of the partial D₂/D₃receptor agonist and α2-adrenoceptor antagonist, piribedil, in the treatment of Parkinson's disease.
  • M. Millan
  • Medicine, Biology
    Pharmacology & therapeutics
  • 2010
TLDR
This paper focuses on the distinctive cellular, preclinical and therapeutic profile of piribedil, comparisons to pramipexole, ropinirole and pergolide, and the core triad of symptoms that characterises PD-motor dysfunction, depressed mood and cognitive impairment.
Neuroprotective effects of the novel D3/D2 receptor agonist and antiparkinson agent, S32504, in vitro against 1-methyl-4-phenylpyridinium (MPP+) and in vivo against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP): a comparison to ropinirole
TLDR
It is demonstrated that S32504 robustly, concentration-dependently and completely protects terminally differentiated SH-SY5Y cells against 1-methyl-4-phenylpyridinium (MPP+)-induced cell death in vitro, and robustly protects dopaminergic neurones against the neurotoxic effects of MPP(+) and MPTP in in vitro and in vivo models, respectively.
S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2 Receptors: II. Actions in Rodent, Primate, and Cellular Models of Antiparkinsonian Activity in Comparison to Ropinirole
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S32504 displays potent and stereospecific activity in rodent, primate, and cellular models of antiparkinsonian properties and engagement of D3 receptors contributes to its neuroprotective properties.
Antidepressant-like properties of the anti-Parkinson agent, piribedil, in rodents: mediation by dopamine D2 receptors
The dopamine D2/D3 receptor agonist and &agr;2 adrenergic receptor antagonist, piribedil, is used clinically as monotherapy and as an adjunct to L-3,4-dihydroxyphenylalanine in the treatment of…
Involvement of dopamine D2/D3 receptors and BDNF in the neuroprotective effects of S32504 and pramipexole against 1-methyl-4-phenylpyridinium in terminally differentiated SH-SY5Y cells
TLDR
S32504 and, less potently, pramipexole show robust, stereospecific, and long-lasting neuroprotective effects against MPP + toxicity that involve D 3 receptors that reflect downstream recruitment of BDNF and via a PK3-AKT pathway.
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