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CTOP
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:103429-31-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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

μ Opioid Receptor/MOR

 

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.
分子量

1062.26

Formula

C50H67N11O11S2

CAS 号

103429-31-8

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.