CTOP TFA 是一种有效的、高选择性的 μ- 阿片受体 (μ-opioid receptor) 拮抗剂。CTOP TFA 可拮抗吗啡诱导的急性镇痛作用和运动亢进。CTOP TFA 提高伏隔核的细胞外多巴胺水平。CTOP TFA 剂量依赖性增强运动能力。
| 生物活性 | CTOP TFA is a potent and highly selectiveμ-opioid receptorantagonist. CTOP TFA antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity[1][2]. |
| IC50& Target | |
体内研究
(In Vivo) | CTOP TFA (0-0.5 nmol, ICV, once) antagonizes the analgesic effect of morphine in a dose-dependent manner[1].
CTOP TFA (0-2 nmol, ICV, once) causes withdrawal hypothermia and a loss of body weight in morphine-dependent animals[1].
CTOP TFA (0-1.5 nmol per side, Intra-VTA injection) enhances extracellular dopamine levels in the nucleus accumbens and dose-dependently enhances locomotor activity[2].
| Animal Model: | Male CFLP mice (25-30 g)[1] | | Dosage: | 0, 0.001, 0.05, 0.075, 0.1, and 0.5 nmol (made up in artificial cerebrospinal
fluid (CSF) and kept in plastic tubes at -25℃ until use) | | Administration: | Intracerebroventricular (i.c.v.) administration, once | | Result: | Antagonized the analgesic effect of morphine in a dose-dependent manner, antagonized
the morphine-induced hypermotility in a dose-dependent manner. |
| Animal Model: | Male CFLP mice (25-30 g, Acute dependence to morphine was induced by a single dependence-inducing (100 mg/kg) dose of morphine-HC1)[1] | | Dosage: | 0, 0.001, 0.05, 0.2, and 2 nmol | | Administration: | Intracerebroventricular (i.c.v.) administration, once | | Result: | Decreased the body temperature in a dose-dependent manner, and caused withdrawal hypothermia and a loss of body weight in morphine-dependent animals. |
| Animal Model: | Long-Evans hooded rats (12, male, 350-450 g)[2] | | Dosage: | 0, 0.015, 0.15, and 1.5 nmol per side | | Administration: | Intra-VTA (ventral tegmental area) injection | | Result: | Enhanced extracellular dopamine levels in the nucleus accumbens, dose-dependently increased activity, whereas had no effect on feeding and drinking behavior. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| Sequence | Phe-Cys-Tyr-Trp-{Orn}-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7) |
| Sequence Shortening | FCYW{Orn}T{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7) |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture and light | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: H2O : 50 mg/mL(42.51 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.8501 mL | 4.2507 mL | 8.5014 mL | | 5 mM | 0.1700 mL | 0.8501 mL | 1.7003 mL | | 10 mM | 0.0850 mL | 0.4251 mL | 0.8501 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 and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (85.01 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
