GLPBio

CTOP

Catalog No.: GC16888Purity:>98.00%
COASDSData Sheet
CTOP es un potente y altamente selectivo antagonista de los receptores opioides μ.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

CTOP
Cas No.: 103429-31-8
1mgIn Stock
$199.00
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5mgIn Stock
$604.00
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10mgIn Stock
$898.00
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25mgIn Stock
$1,629.00
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50mgIn Stock
$2,439.00
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100mgIn Stock
$3,294.00
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Descripción (Description)

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.

Protocolo (Protocol)

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:
[1] 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.
[2] 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.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
103429-31-8
Fórmula molecular
C50H67N11O11S2
Peso molecular
1062.28
Solubilidad
Soluble to 1 mg/ml in Water
Almacenamiento
Desiccate at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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