PD 168077 MALEATE

PD 168077 is a dopamine D₄ receptor agonist (K_i = 8.7 nM in CHO Pro 5 cells expressing the human receptor). It is selective for dopamine D₄ over D₂ and D₃ receptors (K_is = 3,740 and 2,810 nM, respectively), as well as α₁- and α₂-adrenergic and serotonin (5-HT) receptor subtypes 5-HT_1A and 5-HT_2A (K_is = 168, 177, 385, and 4,010 nM, respectively). PD 168077 (20 μM) induces CaMKII translocation from the dendritic shaft to postsynaptic sites on the dendritic processes of primary rat embryonic prefrontal cortex pyramidal neurons, an effect that can be blocked by the IP₃ receptor antagonist 2APB or the calcium chelator BAPTA AM . PD 168077 (50-200 ng/animal) induces penile erections in rats when injected into the paraventricular nucleus (PVN) of the hypothalamus. PD 168077 (0.2-25 mg/kg, s.c.) increases spontaneous locomotor activity and reduces grooming and rearing in rats.

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

A potent D 4 dopamine receptor agonist (K i = 8.7 nM) with > 400-fold selectivity over D 2 and > 300-fold selectivity versus D 3 subtypes respectively. Induces synaptic translocation of CaMK II to postsynaptic sites in cultured prefrontal cortical neurons. Centrally active in vivo .

D₄ Receptor

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[1] Clifford JJ, et al. Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists. Neuropsychopharmacology. 2000 May;22(5):538-44. DOI:10.1016/S0893-133X(99)00141-4
[2] Gu Z, et al. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol Pharmacol. 2006 Mar;69(3):813-22. DOI:10.1124/mol.105.018853