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。
| 生物活性 | CP-809101 hydrochloride is a potent and highly selective5-HT2Creceptor agonist, withpEC50s of 9.96, 7.19 and 6.81 M for human5HT2C,5HT2Band5HT2Areceptor. 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[1][2]. |
| IC50& Target | 5-HT2CReceptor 9.96 (pEC50) | 5-HT2BReceptor 7.19 (pEC50) | 5-HT2AReceptor 6.81 (pEC50) |
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体内研究
(In Vivo) | CP-809101 hydrochloride (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner[1].
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)[1].
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED50value of 2.2 mg/kg[1].
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[2].
| Animal Model: | Male CF rats (conditioned avoidance responding (CAR) model)[1]. | | Dosage: | 0.1-56 mg/kg | | Administration: | Subcutaneous injection; single. | | Result: | Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50value of 4.8 mg/kg. |
| Animal Model: | Male CD rats (PCP or d-amphetamine-induced hyperactivity model)[1]. | | Dosage: | 0.56, 1.78, 5.6, 17.8 mg/kg | | Administration: | Subcutaneous injection; single. | | Result: | Antagonized PCP-induced hyperactivity, with an ED50value of 2.4 mg/kg.
Antagonized d-amphetamine-induced hyperactivity, with an ED50value of 2.7 mg/kg, and in a dose-dependent manner. |
| Animal Model: | Male CD rats (spontaneous locomotor model)[1]. | | 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)[2]. | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 20 mg/mL(58.61 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
