|2-((4-(吡啶-2-基)哌嗪-1-基)甲基)-1H-苯并[d]咪唑|CsnPharm

CAS No.: 70006-24-5

2-((4-(Pyridin-2-yl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole Catalog No. CSN25294

Synonyms: UNII-4WV2575JWT

ABT-724 is a potent and highly selective dopamine D4 receptor agonist with EC50s of 12.4 nM, 14.3 nM and 23.2 nM for human dopamine D4 receptor, rat D4 receptor and ferret D4 receptor.

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技术信息

生物活性

描述Dopamine is the main catecholamine in the central nervous system. The dopamine D₄ receptor is abundantly expressed in the cortex and hypothalamus, and plays a key role in the regulation of sexual function in mammals. ABT-724 is a highly potent, selective dopamine D₄ receptor with an EC50 value of 12.4nM and 61% efficacy for human dopamine D₄ receptor, but shows no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 also exhibits potent but partial agonist effects on rat and ferret D₄ receptors with EC50 values of 14.3±0.6nM and 23.2±1.3nM, respectively. Subcutaneous injection of ABT-724 at doses of 0.01, 0.03, 0.1, 0.3, and 1μmol/kg induced significant facilitation of penile erection in rats. The maximal effect was observed at 0.03μmol/kg with a 77% incidence, compared to 23% incidence in the control group. The latency to induce a penile erection in ABT-724-treated rats was 18.7 minutes. Also in rats with chronically implanted cannulas, injection of ABT-724 directly into the lateral ventricle significantly facilitated erectile responses at 3nmol. Subcutaneous administration of ABT-724 at 0.0025μmol/kg resulted in 2.0±0.6 episodes of increase in intracavernous pressure in an awake freely moving rat.^[1]
作用机制ABT-724 is a selective dopamine D₄ receptor agonist that facilitates penile erection in rats without affecting cardiovascular, gastrointestinal, or central nervous system function.^[1]
参考文献

[1] Brioni JD, Moreland RB, Cowart M, Hsieh GC, Stewart AO, Hedlund P, Donnelly-Roberts DL, Nakane M, Lynch JJ 3rd, Kolasa T, Polakowski JS, Osinski MA, Marsh K, Andersson KE, Sullivan JP. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6758-63. doi: 10.1073/pnas.0308292101

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
- 3.4087 mL
- 17.0435 mL
- 34.0871 mL
- 5 mM
- 0.6817 mL
- 3.4087 mL
- 6.8174 mL
- 10 mM
- 0.3409 mL
- 1.7044 mL
- 3.4087 mL

技术信息

CAS号	70006-24-5	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C17H19N5	运输	蓝冰
分子量	293.37	别名	UNII-4WV2575JWT

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2-((4-(Pyridin-2-yl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole Catalog No. CSN25294

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