| 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
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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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