CTOP是一种强效且高选择性的μ-opioid受体拮抗剂，IC50值为2.80nM。
Cas No.:103429-31-8
Sample solution is provided at 25 µL, 10mM.
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CTOP is a potent and highly selective μ-opioid receptor antagonist with an IC50 value of 2.80nM [1]. CTOP can regulate the peptide release at the nerve pitulette terminals of rats by targeting the μ-opioid receptor and blocking the inhibition of Ca2+ influx[2]. CTOP has been widely used to regulate the body temperature and weight of mouse models as well as to block the analgesic effect caused by morphine[3].
In vitro, CTOP treatment (10nM) for 48 hours significantly inhibited the cytotoxicity of delta opioid peptide [D-Ala2, D-Leu5]enkephalin (DADLE) on PC12 cells and promoted cell survival[4]. The 15-minute treatment with CTOP (1µM) completely blocked the inhibitory effect of morphine and remifentanil on the elevated lactate dehydrogenase (LDH) activity in the isolated failing rat hearts[5].
In vivo, CTOP treatment (1mg/kg) via intraperitoneal injection 15 minutes before drinking significantly reduced the alcohol intake in alcohol-preferring C57BL/6 mice [6]. Thirty minutes before the heat plate test, a single dose of CTOP (6µg/rat) was injected into the rostral anterior cingulate cortex (rACC) of the rats, which could reduce the pain threshold in placebo analgesia rats [7].
References:
[1] Gulya K, Lui G K, Pelton J T, et al. HD-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2: A potent and selective antagonist for mu opioid receptors[J]. Progress in Opioid Research, 1986: 209.
[2] Ortiz‐Miranda S I, Dayanithi G, Coccia V, et al. µ‐Opioid Receptor Modulates Peptide Release From Rat Neurohypophysial Terminals By Inhibiting Ca2+ Influx[J]. Journal of neuroendocrinology, 2003, 15(9): 888-894.
[3] Gulya K, Kriván M, Nyolczas N, et al. Central effects of the potent and highly selective μ opioid antagonist (CTOP) in mice[J]. European journal of pharmacology, 1988, 150(3): 355-360.
[4] Hayashi T, Tsao L I, Su T P. Antiapoptotic and cytotoxic properties of delta opioid peptide [D‐Ala2, D‐Leu5] enkephalin in PC12 cells[J]. Synapse, 2002, 43(1): 86-94.
[5] He S F, Jin S Y, Yang W, et al. Cardiac μ-opioid receptor contributes to opioid-induced cardioprotection in chronic heart failure[J]. British journal of anaesthesia, 2018, 121(1): 26-37.
[6] Kim S G, Stromberg M F, Kim M J, et al. The effect of antagonists selective for μ-and δ-opioid receptor subtypes on alcohol consumption in C57BL/6 mice[J]. Alcohol, 2000, 22(2): 85-90.
[7] Zhang R R, Zhang W C, Wang J Y, et al. The opioid placebo analgesia is mediated exclusively through µ-opioid receptor in rat[J]. International Journal of Neuropsychopharmacology, 2013, 16(4): 849-856.
CTOP是一种强效且高选择性的μ-opioid受体拮抗剂，IC50值为2.80nM[1]。CTOP可通过靶向μ-阿片受体并阻断Ca2+内流的抑制作用，调节大鼠神经垂体末梢的肽类释放[2]。CTOP已被广泛用于调节小鼠模型的体温和体重，以及阻断吗啡引起的镇痛作用[3]。
在体外，使用10nM的CTOP处理PC12细胞48小时，显著抑制了delta opioid peptide [D-Ala2, D-Leu5]enkephalin (DADLE)的细胞毒性，并促进了细胞存活[4]。使用1µM的CTOP处理15分钟，完全阻断了吗啡和瑞芬太尼对离体衰竭大鼠心脏中乳酸脱氢酶（LDH）活性升高的抑制作用[5]。
在体内，偏好饮酒的C57BL/6小鼠在饮酒前15分钟腹腔注射1mg/kg剂量的CTOP，可显著减少酒精摄入量[6]。在热板试验前30分钟，将单剂量6µg/只大鼠的CTOP注入大鼠的前喙扣带皮质（rACC），可降低安慰剂镇痛大鼠的痛阈[7]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | PC12 cells were cultured at 37°C, 5% CO2 on collagen-coated flasks with RPMI1640 medium containing 5% fetal calf serum, 10% horse serum, glutamine (4mM), penicillin (50U/ml) and streptomycin (50mg/ml). Cells were washed four times with serum-free medium and were cultured in serum-free conditions for 48h with DADLE (100pM) with or without CTOP (10nM). Then, analyze the cell viability. |
Reaction Conditions | 10nM; 48h |
Applications | CTOP treatment significantly enhanced the cell viability of PC12 cells after treatment with DADLE. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Male C57BL/6 mice (3-week-old) were housed five to a cage and allowed to adapt for 5 days after arrival. Water and food were available ad lib. For 7 days, the mice were forced to drink an alcohol solution (10% v/v) with continued ad lib. access to food. From days 8 to 35, each mouse was housed in an individual cage with food available ad lib. and water available for 22h, and an alcohol solution (10% v/v) available for the remaining 2h. Daily intake of food (24h) and water (22h) was tabulated by weighing the food and water bottles to the nearest 0.01g every day before presentation of the alcohol bottle. Similarly, the alcohol bottle was weighed both at the start and at the end of the 2h access period. Mice were also weighed at this time. At the end of day 33, mice were matched for alcohol consumption and randomly assigned to one of five groups. The matching procedure involved ranking mice according to their mean baseline alcohol consumption. The five mice with the highest consumption were distributed across the five experimental groups, etc. This ensured comparable alcohol consumption across the groups. Mice in group CTOP (n=7) received intraperitoneal injections of CTOP 1mg/kg. All saline or CTOP injections were administered 15min before access to alcohol on day 35. Analyze the alcohol intake within 2 hours of CTOP consumption. |
Dosage form | 1mg/kg for once; i.p. |
Applications | CTOP treatment significantly inhibited alcohol consumption in alcohol-preferring C57BL/6 mice. |
References: | |
| Cas No. | 103429-31-8 | SDF | |
| 分子式 | C50H67N11O11S2 | 分子量 | 1062.28 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Desiccate at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 941.4 μL | 4.7069 mL | 9.4137 mL |
| 5 mM | 188.3 μL | 941.4 μL | 1.8827 mL |
| 10 mM | 94.1 μL | 470.7 μL | 941.4 μL |
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