The preferential dopamine D3 receptor ligand, (+)-UH232, is a partial agonist

Eur J Pharmacol. 1995 Aug 25;282(1-3):R3-4. doi: 10.1016/0014-2999(95)00460-3.

Abstract

In a NG 108 15 hybrid cell line stably expressing a recombinant dopamine D3 receptor, (+)-UH 232 (cis-(+)-1S,2R)-5-methoxy-1-methyl-2-(di-n- propylamino)tetralin), a partially selective D3 receptor ligand, stimulates mitogenesis, as measured by incorporation of [3H]thymidine, with an EC50 of 7.6 nM and a maximal increase corresponding to 23% of the response elicited by quinpirole, a full agonist. This effect was antagonised by nafadotride, a D3 receptor-selective antagonist. (+)-UH 232 also antagonised quinpirole-induced mitogenesis with a Ki value of 9.4 nM. (+)-UH 232 (1 microM) inhibited by 22% the forskolin-induced accumulation of cAMP, whilst the inhibition by quinpirole (100 nM) was 53%. These results indicate that (+)-UH 232 is a partial agonist at the D3 receptor with an intrinsic activity of 0.2-0.4.

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin / analogs & derivatives*
  • 8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
  • Ergolines / pharmacology
  • Humans
  • Hybrid Cells
  • Mitogens / pharmacology
  • Quinpirole
  • Receptors, Dopamine / biosynthesis
  • Receptors, Dopamine / drug effects*
  • Receptors, Dopamine / genetics
  • Receptors, Dopamine D2*
  • Receptors, Dopamine D3
  • Recombinant Proteins / biosynthesis

Substances

  • DRD3 protein, human
  • Ergolines
  • Mitogens
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • Recombinant Proteins
  • Quinpirole
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • UH 232