CTOP 是一种有效的、高选择性的 μ- 阿片受体 (μ-opioid receptor) 拮抗剂。CTOP 可拮抗吗啡诱导的急性镇痛作用和运动亢进。CTOP 提高伏隔核的细胞外多巴胺水平。CTOP 剂量依赖性增强运动能力。
| 生物活性 | CTOP is a potent and highly selectiveμ-opioid receptorantagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity[1][2]. |
| IC50& Target | |
体内研究
(In Vivo) | CTOP (0-0.5 nmol, ICV, once) antagonizes the analgesic effect of morphine in a dose-dependent manner[1].
CTOP (0-2 nmol, ICV, once) causes withdrawal hypothermia and a loss of body weight in morphine-dependent animals[1].
CTOP (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. |
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| 分子量 | |
| Formula | |
| CAS 号 | |
| 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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
