PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively.
In vivo, PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual and characteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes of myoclonic jerking; grooming, and rearing are reduced.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
Bidirectional modulation of hippocampal synaptic plasticity by Dopaminergic D4-receptors in the CA1 area of hippocampus.
Navakkode S, et al. Sci Rep. 2017 Nov 14;7(1):15571. PMID: 29138490.
Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons.
Gu Z, et al. Mol Pharmacol. 2006 Mar;69(3):813-22. PMID: 16365279.
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