Drug intelligence / Profile preview

PD168077

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intraperitoneal, Subcutaneous, Intracerebroventricular, Experimental (animal Studies)
01

Overview

PD168077 is a potent and selective small molecule agonist of the dopamine D4 receptor, with a Ki of 8.7 nM and >400-fold selectivity over D2 and >300-fold over D3 dopamine receptor subtypes[1][9][6]. It is used primarily as a research tool to investigate D4 receptor pharmacology and function, particularly in neurobiological and behavioral studies. PD168077 has been shown to induce penile erection in animal models by acting on D4 receptors in the paraventricular nucleus of the hypothalamus and increasing central oxytocinergic neurotransmission, with involvement of nitric oxide pathways[3][4][7]. It is centrally active in vivo and has also been used in studies related to synaptic effects in prefrontal cortical neurons.

Other names
N-((4-(2-cyanophenyl)piperazin-1-yl)methyl)-3-methylbenzamide maleate
02

Targets

DRD4 (Dopamine D4 Receptor)

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