PD 168077 MALEATE
- Product Name
- PD 168077 MALEATE
- CAS No.
- 630117-19-0
- Chemical Name
- PD 168077 MALEATE
- Synonyms
- PD 168077 (maL;PD 168077 MALEATE;PD-168077 maleate, 10 mM in DMSO;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);PD 168077,Dopamine Receptor,PD-168077,inhibit,PD168077,PD168077 maleate,Inhibitor,PD 168077 maleate
- CBNumber
- CB6679671
- Molecular Formula
- C24H26N4O5
- Formula Weight
- 450.49
- MOL File
- Mol file
PD 168077 MALEATE Property
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- DMSO: >10 mg/mL
- form
- powder
- color
- white
Safety
- Safety Statements
- 22-24/25
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 5.05878
- Product name
- PD 168077 Maleate - CAS 630117-19-0 - Calbiochem
- Packaging
- 10mg
- Price
- $207
- Updated
- 2025/07/31
- Product number
- 29789
- Product name
- PD 168077 (maleate)
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 29789
- Product name
- PD 168077 (maleate)
- Packaging
- 50mg
- Price
- $638
- Updated
- 2024/03/01
- Product number
- 29789
- Product name
- PD 168077 (maleate)
- Packaging
- 10mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 29789
- Product name
- PD 168077 (maleate)
- Packaging
- 25mg
- Price
- $365
- Updated
- 2024/03/01
PD 168077 MALEATE Chemical Properties,Usage,Production
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
PD 168077 MALEATE Preparation Products And Raw materials
Raw materials
Preparation Products
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