RU 24969是一种广泛使用的非选择性5-HT1B/1A激动剂，其对5-HT1B受体的Ki值为0.38nM，对5-HT1A受体的Ki值为2.5nM，而对大脑中的其他受体位点亲和力较低。
Cas No.:66611-26-5
Sample solution is provided at 25 µL, 10mM.
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RU 24969 is a widely used nonselective 5-HT1B/1A agonist with a Ki value of 0.38nM for the 5-HT1B receptor and 2.5nM for the 5-HT1A receptor, but with lower affinity for other receptor sites in the brain[1]. RU 24969 induces robust hyperlocomotor activity, characterized by increased forward locomotion and a concomitant reduction in fluid consumption[1].
In vitro, 10μM RU-24969 attenuated 21mM K⁺-induced [³H]-5-HT release in cultured rat frontal cortex slices, reducing it by approximately 30%[2].
In vivo, subcutaneous administration of RU 24969 at doses of 0.3, 1, and 3mg/kg produced a dose-dependent reduction in water intake in male SD rats within a 30-45min observation period. In addition, subcutaneous administration of RU 24969 (3mg/kg) significantly increased total forward locomotion within 15-45min after dosing[1]. Administration of RU-24969 at 10mg/kg by intraperitoneal injection decreased extracellular 5-HT and its metabolite, 5-hydroxyindoleacetic acid (5-HIAA) in rats[2].
References:
[1] Aronsen D, Webster J, Schenk S. RU 24969-produced adipsia and hyperlocomotion: differential role of 5HT 1A and 5HT 1B receptor mechanisms. Pharmacol Biochem Behav. 2014;124:1-4.
[2] Brazell MP, Marsden CA, Nisbet AP, Routledge C. The 5-HT1 receptor agonist RU-24969 decreases 5-hydroxytryptamine (5-HT) release and metabolism in the rat frontal cortex in vitro and in vivo. Br J Pharmacol. 1985;86(1):209-216.
RU 24969是一种广泛使用的非选择性5-HT1B/1A激动剂，其对5-HT1B受体的Ki值为0.38nM，对5-HT1A受体的Ki值为2.5nM，而对大脑中的其他受体位点亲和力较低[1]。RU 24969可显著诱导过度运动，同时表现为向前运动增加及液体摄入减少[1]。
体外实验中，10μM RU-24969可显著抑制21mM K⁺诱导的培养大鼠额叶皮质切片中[³H]-5-HT的释放，抑制幅度约为30%[2]。
体内实验中，皮下注射0.3、1和3mg/kg剂量的RU 24969，在30-45分钟的观察时间内雄性SD大鼠的饮水量呈剂量依赖性降低。皮下注射3mg/kg RU 24969可在15-45分钟内显著提高大鼠总向前运动水平[1]。腹腔注射10mg/kg的RU-24969可显著降低大鼠细胞外5-HT及其代谢产物5-羟基吲哚乙酸（5-HIAA）的水平[2]。
| Animal experiment [1]: | |
Animal models | Male Sprague–Dawley rats |
Preparation Method | Water bottles were removed and 23.75h later, RU 24969 (0-3mg/kg, s.c.) was administered. The water bottles were reintroduced 15min after the RU 24969 injection. Consumption was measured for a 30min period. Fluid consumption was determined by weighing water bottles before and after the test. |
Dosage form | 0.3, 1, 3mg/kg; once; s.c. |
Applications | Administration of 0.3, 1 and 3mg/kg resulted in a dose-dependent reduction in water intake. |
References: | |
| Cas No. | 66611-26-5 | SDF | |
| Canonical SMILES | COC1=CC=C2C(C(C3=CCNCC3)=CN2)=C1 | ||
| 分子式 | C14H16N2O | 分子量 | 228.29 |
| 溶解度 | DMSO: ≥ 30 mg/mL (131.41 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3804 mL | 21.902 mL | 43.8039 mL |
| 5 mM | 876.1 μL | 4.3804 mL | 8.7608 mL |
| 10 mM | 438 μL | 2.1902 mL | 4.3804 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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