产品介绍 |
CP-809101 hydrochloride 是一种强效的,高选择性的 5-HT2C 受体激动剂,其对人 5HT2C, 5HT2B 和 5HT2A 受体的 pEC50 值分别为 9.96, 7.19 和 6.81 M。CP-809101 hydrochloride 能抑制大鼠的条件回避反应,以及 phencyclidine hydrochloride 和 d-amphetamine 诱导的多动症,还能减少大鼠对食物和尼古丁的依赖,可用于抗精神病以及尼古丁依赖的研究。
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生物活性 |
CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.
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体外研究 | |
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体内研究 |
CP-809101 hydrochloride (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner.
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner).
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED50 value of 2.2 mg/kg.
CP-809101 hydrochloride (0.3, 1, 3 mg/kg; s.c.; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Male CF rats (conditioned avoidance responding (CAR) model). |
Dosage: |
0.1-56 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg. |
Animal Model: |
Male CD rats (PCP or d-amphetamine-induced hyperactivity model). |
Dosage: |
0.56, 1.78, 5.6, 17.8 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg.
Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner.
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Animal Model: |
Male CD rats (spontaneous locomotor model). |
Dosage: |
0.56, 1.78, 5.6, 17.8 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg). |
Animal Model: |
Adult male Sprague-Dawley rats (280-400 g). |
Dosage: |
0.3, 1, 3 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Produced a dose-related decrease in responding for food and nicotine self-administration in rats. |
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体内研究 |
CP-809101 hydrochloride (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner.
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner).
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED50 value of 2.2 mg/kg.
CP-809101 hydrochloride (0.3, 1, 3 mg/kg; s.c.; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Male CF rats (conditioned avoidance responding (CAR) model). |
Dosage: |
0.1-56 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg. |
Animal Model: |
Male CD rats (PCP or d-amphetamine-induced hyperactivity model). |
Dosage: |
0.56, 1.78, 5.6, 17.8 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg.
Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner.
|
Animal Model: |
Male CD rats (spontaneous locomotor model). |
Dosage: |
0.56, 1.78, 5.6, 17.8 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg). |
Animal Model: |
Adult male Sprague-Dawley rats (280-400 g). |
Dosage: |
0.3, 1, 3 mg/kg |
Administration: |
Subcutaneous injection; single. |
Result: |
Produced a dose-related decrease in responding for food and nicotine self-administration in rats. |
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性状 | Solid |
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溶解性数据 |
In Vitro:
H2O : 20 mg/mL (58.61 mM; Need ultrasonic)
配制储备液
浓度
溶剂体积
质量
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1 mg |
5 mg |
10 mg |
1 mM |
2.9305 mL |
14.6524 mL |
29.3049 mL |
5 mM |
0.5861 mL |
2.9305 mL |
5.8610 mL |
10 mM |
0.2930 mL |
1.4652 mL |
2.9305 mL |
*
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
4°C, sealed storage, away from moisture
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参考文献 | |
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