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Antipsychotics & D3, D4

Key message: most antipsychotic drugs interact with dopamine D3 and D4 receptors. Activity at these sites may improve cognition and reduce EPS.

  • Antipsychotics generally interact with D3 receptors wih similar affinity as at D2. Affinity at D4 receptors is more diverse, with clozapine exhibiting reinforced affinity.
  • The in vitro signal transduction (G-protein and MAPK activation) profile of D3 receptors differs from that of D2 receptors.
  • S33138 (Ph.II, discontinued), a preferential D3 vs D2 antagonist, exhibits favorable antipsychotic-like and cognitive properties in rodents.
  • Partial agonism at D4 receptors opposes scopolamine-induced social recognition deficit in rodents (similarly to effects observed by others with D3 antagonists).
  • D4 receptors exhibit "promiscuous" interaction with adrenaline and noradrenaline: the latter act as potent D4 agonists.
# Article Title
1 Antipsychotic, antidepressant, and cognitive-impairment properties of antipsychotics: rat profile and implications for behavioral and psychological symptoms of dementia.
2 ADN-1184 a monoaminergic ligand with 5-HT6/7 receptor antagonism: pharmacological profile and potential therapeutic utility.
3 G protein activation by human dopamine D3 receptors in high-expressing Chinese hamster ovary cells: A guanosine-5'-O-(3-[35S]thio)- triphosphate binding and antibody study. PDF
4 Human dopamine D3 receptors mediate mitogen-activated protein kinase activation via a phosphatidylinositol 3-kinase and an atypical protein kinase C-dependent mechanism. PDF
5 The novel antagonist, S33084, and GR218,231 interact selectively with cloned and native, rat dopamine D3 receptors as compared with native, rat dopamine D2 receptors.
6 S33138, a preferential dopamine D3 versus D2 receptor antagonist and potential antipsychotic agent: I. Receptor-binding profile and functional actions at G-protein-coupled receptors. PDF
7 Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors.
8 [3H]S33084: a novel, selective and potent radioligand at cloned, human dopamine D3 receptors.
9 Noradrenaline and adrenaline are high affinity agonists at dopamine D4 receptors.
10 Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells.
11 S18126, a potent, selective and competitive antagonist at dopamine D4 receptors: an in vitro and in vivo comparison with L 745,870 and raclopride. PDF
12 [35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents. PDF
13 A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D3 receptor antagonists (+)-S14297, nafadotride, GR103,691 and U99194. PDF
14 S33084, a novel, potent, selective, and competitive antagonist at dopamine D3-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. PDF
15 [3H](+)S 14297: a novel, selective radioligand at cloned human dopamine D3 receptors.
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