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PD-168077 maleate

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Chemical Structure| 630117-19-0 同义名 : PD 168077 (maleate)
CAS号 : 630117-19-0
货号 : A447591
分子式 : C24H26N4O5
纯度 : 98%+
分子量 : 450.49
MDL号 : MFCD01321067
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(321.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.20mL

4.44mL

2.22mL
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