| Identification | Back Directory | [Name]
PD 168077 MALEATE | [CAS]
630117-19-0 | [Synonyms]
PD 168077 (maL
PD 168077 MALEATE
N-(METHYL-4-(2-CYANOPHENYL)PIPERAZINYL)-3-METHYLBENZAMIDE MALEATE
N-[[4-(2-CYANOPHENYL)-1-PIPERAZINYL]METHYL]-3-METHYL-BENZAMIDE MALEATE
Benzamide,N-[[4-(2-cyanophenyl)-1-piperazinyl]methyl]-3-methyl-,(2Z)-2-butenedioate(1:1) | [Molecular Formula]
C24H26N4O5 | [MDL Number]
MFCD01321067 | [MOL File]
630117-19-0.mol | [Molecular Weight]
450.49 |
| Hazard Information | Back Directory | [Description]
PD 168077 is a dopamine D4 receptor agonist (Ki = 8.7 nM in CHO Pro 5 cells expressing the human receptor). It is selective for dopamine D4 over D2 and D3 receptors (Kis = 3,740 and 2,810 nM, respectively), as well as α1- and α2-adrenergic and serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2A (Kis = 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. | [Uses]
PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM. | [Biological Activity]
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 . | [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[1]. | [IC 50]
D4 Receptor | [storage]
Store at -20°C | [References]
[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 |
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