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| | PD 168077 MALEATE Basic information |
| Product Name: | PD 168077 MALEATE | | Synonyms: | N-(METHYL-4-(2-CYANOPHENYL)PIPERAZINYL)-3-METHYLBENZAMIDE MALEATE;PD 168077 MALEATE;N-[[4-(2-CYANOPHENYL)-1-PIPERAZINYL]METHYL]-3-METHYL-BENZAMIDE MALEATE;PD 168077 (maL;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 | | CAS: | 630117-19-0 | | MF: | C24H26N4O5 | | MW: | 450.49 | | EINECS: | | | Product Categories: | | | Mol File: | Mol File |  |
| | PD 168077 MALEATE Chemical Properties |
| storage temp. | Inert atmosphere,2-8°C | | solubility | DMSO: >10 mg/mL | | form | powder | | color | white |
| | PD 168077 MALEATE Usage And Synthesis |
| 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. | | 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 . | | storage | Store at -20°C |
| | PD 168077 MALEATE Preparation Products And Raw materials |
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