Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization.

@article{Millan2001AntiparkinsonianAP,
  title={Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization.},
  author={Mark John Millan and Didier Cussac and Graeme Milligan and Catherine Carr and Val{\'e}rie Audinot and Alain P Gobert and Françoise Lejeune and J M Rivet and Mauricette Brocco and Delphine Duqueyroix and Jean Paul Nicolas and Jean A. Boutin and Adrian Newman-Tancredi},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2001},
  volume={297 3},
  pages={876-87}
}
Compared with cloned, human (h)D(2) receptors (pK(i) = 6.9), the antiparkinsonian agent piribedil showed comparable affinity for halpha(2A)- (7.1) and halpha(2C)- (7.2) adrenoceptors (ARs), whereas its affinity for halpha(2B)-ARs was less marked (6.5). At halpha(2A)- and halpha(2C)-ARs, piribedil antagonized induction of [(35)S]guanosine-5'-O-(3-thio)triphosphate (GTPgammaS) binding by norepinephrine (NE) with pK(b) values of 6.5 and 6.9, respectively. Furthermore, Schild analysis of the… CONTINUE READING

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