CTOP |
Catalog No.GC16888
One-Click Copy Product Info
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CTOP es un potente y altamente selectivo antagonista de los receptores opioides μ.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Formula | C50H67N11O11S2 | M.Wt | 1062.28 |
| Solubility | Soluble to 1 mg/ml in Water | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)