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630117-19-0

630117-19-0 structure
630117-19-0 structure
  • Name: PD 168077 maleate
  • Chemical Name: N-{[4-(2-Cyanophenyl)-1-piperazinyl]methyl}-3-methylbenzamide (2Z)-2-butenedioate (1:1)
  • CAS Number: 630117-19-0
  • Molecular Formula: C24H26N4O5
  • Molecular Weight: 450.487
  • Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
  • Create Date: 2018-01-23 09:48:29
  • Modify Date: 2024-01-14 15:16:13
  • PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

Name N-{[4-(2-Cyanophenyl)-1-piperazinyl]methyl}-3-methylbenzamide (2Z)-2-butenedioate (1:1)
Synonyms N-{[4-(2-Cyanophenyl)-1-piperazinyl]methyl}-3-methylbenzamide (2Z)-2-butenedioate (1:1)
N-{[4-(2-Cyanophenyl)piperazin-1-yl]methyl}-3-methylbenzamide (2Z)-but-2-enedioate (1:1)
Benzamide, N-[[4-(2-cyanophenyl)-1-piperazinyl]methyl]-3-methyl-, (2Z)-2-butenedioate (1:1)
Description PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
Related Catalog
Target

Ki: 9 nM (Dopamine D4 receptor)[1].

In Vitro PD-168077 is one of the first agents to be identified as putative selective D4 agonists. It shows >100-fold selectivity over other members of the D2-like receptor family and over their D1-like counterparts; PD-168077 shows a 20-fold selectivity over α1, and α2, a 45-fold selectivity over 5-HT1A, and a 460-fold selectivity over 5-HT2A receptors; PD-168077 evidences intrinsic activity at the D4 receptor in terms of quinpirole-like inhibition of forskolin-stimulated cAMP accumulation or stimulation of [3H]thymidine uptake in CHO cells expressing the human D4 receptor[1]. In the PD-168077-treated cell, p-CaMKII exhibits a significantly increased clustering at synaptic sites, as indicated by the enhanced colocalization with PSD-95[2].
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].
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.

[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.

Molecular Formula C24H26N4O5
Molecular Weight 450.487
Exact Mass 450.190308
Storage condition 2-8℃