PD 168077 МАЛЕАТ

Описание

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.

Биологическая активность

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 .