630117-19-0|N-((4-(2-Cyanophenyl)piperazin-1-yl)methyl)-3-methylbenzamide maleate|CsnPharm

CAS No.: 630117-19-0

PD-168077 maleate Catalog No. CSN23271

Synonyms: PD 168077 (maleate);PD-168077;PD-168,077

PD 168077 maleate is an agonist of D4 dopamine receptor with Ki of 8.7 nM. It can induce synaptic translocation of CaMK II to postsynaptic sites in cultured prefrontal cortical neurons.

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技术信息

生物活性

描述PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM. PD 168077 (0.2-25.0 mg/kg) induced nonstereotyped shuffling locomotion with uncoordinated movements, jerking, and yawning, which were insensitive to antagonism by CP-293,019, L-745,870, or haloperidol^[1]. 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]. PD-168077 (1-200 ng) induced penile erection in a dose-dependent manner. The minimal effective dose was 50 ng, while the maximal response was found with 200 ng of the compound, which increased penile erection episodes from 0.3+/-0.03 to 1.7+/-0.21^[3]. Apomorphine (0.1microg) and PD-168077 (0.1microg) induced penile erection episodes, which occurred concomitantly to an increase in extra-cellular dopamine and DOPAC (3,4-dihydroxyphenylacetic acid) concentration in the dialysate from the shell of the nucleus accumbens, as measured by intracerebral microdialysis. Stimulation of dopamine receptors (mainly of the D2 to D4 subtype) in the paraventricular nucleus induces the release of oxytocin in brain areas that influence the activity of mesolimbic dopaminergic neurons mediating the appetitive and reinforcing effects of sexual activity^[4].
参考文献

[1] Clifford JJ, Waddington JL. Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists. Neuropsychopharmacology. 2000;22(5):538‐544
[2] Gu Z, Jiang Q, Yuen EY, Yan Z. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol Pharmacol. 2006;69(3):813‐822
[3] Melis MR, Succu S, Mascia MS, Argiolas A. PD-168077, a selective dopamine D4 receptor agonist, induces penile erection when injected into the paraventricular nucleus of male rats. Neurosci Lett. 2005;379(1):59‐62
[4] Succu S, Sanna F, Melis T, Boi A, Argiolas A, Melis MR. Stimulation of dopamine receptors in the paraventricular nucleus of the hypothalamus of male rats induces penile erection and increases extra-cellular dopamine in the nucleus accumbens: Involvement of central oxytocin. Neuropharmacology. 2007;52(3):1034‐1043

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2198 mL
- 11.0990 mL
- 22.1981 mL
- 5 mM
- 0.4440 mL
- 2.2198 mL
- 4.4396 mL
- 10 mM
- 0.2220 mL
- 1.1099 mL
- 2.2198 mL

技术信息

CAS号

630117-19-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H26N4O5

运输

蓝冰

分子量

450.49

别名

PD 168077 (maleate);PD-168077;PD-168,077

溶解度

DMSO	240.0 mg/mL (532.8 mM)
Water	insoluble

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PD-168077 maleate Catalog No. CSN23271

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