PD-168077 maleate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PD-168077 马来酸盐是多巴胺 D4 受体的选择性激动剂 (Ki : 9 nM) PD-168077 是一种选择性 D4 多巴胺受体激动剂，注射到下丘脑的室旁核中，对雄性大鼠的阴茎勃起进行了研究。 PD-168077 (1-200 ng) 以剂量依赖性方式诱导阴茎勃起。

PD-168077 maleate is a selective agonist of dopamine D4 receptor(Ki : 9 nM)PD-168077, a selective D4 dopamine receptor agonist, injected into the paraventricular nucleus of the hypothalamus on penile erection was studied in male rats.?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.?The proerectile effect of PD-168077 was reduced almost completely by L-745,870 (3-(4-[chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-B]pyridine trihydrochloride), a selective D4 dopamine receptor antagonist, (1 microg) given into the paraventricular nucleus before the D4 dopamine agonist, and by other nonselective dopamine receptor antagonists, such as haloperidol (1 microg) and clozapine (1 microg), which block all dopamine receptor subtypes.?The pro-erectile effect of PD-168077 was also reduced by the NO synthase inhibitor NG-nitro-L-arginine methylester (25 microg), but not by the oxytocin receptor antagonist d(CH2)5Tyr(Me)2-Orn8-vasotocin (1 microg), when given into the paraventricular nucleus.?In spite of its inability to prevent the pro-erectile effect of PD-168077 when given in the paraventricular nucleus, d(CH2)5Tyr(Me)2-Orn8-vasotocin (1 microg) reduced almost completely PD-168077-induced penile erection when given into the lateral ventricles.?

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GPCR/G Protein

Dopamine Receptor

D4

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630117-19-0

450.49

C24H26N4O5

>98% (HPLC)

DMSO:150 mg/mL (332.97 mM; Need ultrasonic)

O=C(NCN1CCN(C2=CC=CC=C2C#N)CC1)C3=CC=CC(C)=C3.O=C(O)/C=C\C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years