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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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.
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