A functional test identifies dopamine agonists selective for D3 versus D2 receptors

Neuroreport. 1995 Jan 26;6(2):329-32. doi: 10.1097/00001756-199501000-00026.


The functional potency of a series of dopamine agonists for increasing mitogenesis, measured by incorporation of [3H]thymidine, was established in transfected cell lines expressing human D2 or D3 receptors. The functional selectivity of agonists markedly differs from their binding selectivity. (+)7-OH-DPAT, pramipexole, quinerolane and PD 128,907, the most D3 receptor-selective compounds in binding studies, were 7, 15, 21 and 54 times more potent, respectively, at the D3 than at the D2 receptor in the functional test. Bromocriptine displayed a 10-fold functional selectivity toward the D2 receptor. The known behavioural actions of D3 selective agonists support a role for the D3 receptor in motor inhibitions, which should be taken into account for the treatment of motor dysfunctions by dopamine agonists.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Dopamine Agents / pharmacology*
  • Humans
  • Receptors, Dopamine / drug effects*
  • Receptors, Dopamine D2 / agonists*
  • Receptors, Dopamine D3


  • DRD3 protein, human
  • Dopamine Agents
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3