Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.

@article{Mottola2002FunctionalSO,
  title={Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.},
  author={David M. Mottola and Jason D. Kilts and Mechelle M Lewis and Hilary S Connery and Q. David Walker and Sara R. Jones and Raymond G. Booth and Deborah K. Hyslop and M. F. Piercey and R. Mark Wightman and Cindy P. Lawler and David E. Nichols and Richard B. Mailman},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2002},
  volume={301 3},
  pages={
          1166-78
        }
}
  • D. MottolaJ. Kilts R. Mailman
  • Published 1 June 2002
  • Biology, Chemistry
  • The Journal of pharmacology and experimental therapeutics
Dihydrexidine (DHX), the first high-affinity D(1) dopamine receptor full agonist, is only 10-fold selective for D(1) versus D(2) receptors, having D(2) affinity similar to the prototypical agonist quinpirole. The D(2) functional properties of DHX and its more D(2) selective analog N-n-propyl-dihydrexidine (PrDHX) were explored in rat brain and pituitary. DHX and PrDHX had binding characteristics to D(2) receptors in rat striatum typical of D(2) agonists, binding to both high- and low-affinity… 

Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs.

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Functional selectivity of D2 receptor ligands in a Chinese hamster ovary hD2L cell line: evidence for induction of ligand-specific receptor states.

These findings indicate that DHX, DNS, RNPA, and SNPA have atypical functional properties at the hD(2L) receptor and display different patterns of functional selectivity.

Discovery of D 1 Dopamine Receptor Positive Allosteric Modulators : Characterization of Pharmacology and Identification of Residues that Regulate Species Selectivity s

The present studies represent the first published report of a dopamine D1 positive allosteric modulator (PAM) and define critical amino acids that regulate species selectivity.

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The present studies represent the first published report of a dopamine D1 positive allosteric modulator (PAM). D1 receptors have been proposed as a therapeutic target for the treatment of cognitive
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