2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. CTOP TFA

CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

CTOP TFA Chemical Structure

CTOP TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

Other Forms of CTOP TFA:

CTOP TFA Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CTOP TFA

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity[1][2].

IC50 & Target

μ Opioid Receptor/MOR

 

In Vivo

CTOP TFA (0-0.5 nmol, ICV, once) antagonizes the analgesic effect in a dose-dependent manner[1].
CTOP TFA (0-2 nmol, ICV, once) causes withdrawal hypothermia and a loss of body weight in animals[1].
CTOP TFA (0-1.5 nmol per side, Intra-VTA injection) enhances extracellular dopamine levels in the nucleus accumbens and dose-dependently enhances locomotor activity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 in a dose-dependent manner, antagonized the 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 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.
Molecular Weight

1062.27 (free base)

Formula

OC(C(F)(F)F)=O.O=C(N[C@@H]1CC2=CNC3=CC=CC=C23)[C@H](CC4=CC=C(O)C=C4)NC([C@@H](NC([C@@H](CC5=CC=CC=C5)N)=O)CSSC([C@@H](C(N[C@@H]([C@@H](C)O)C(N)=O)=O)NC([C@]([H])([C@@H](C)O)NC([C@H](CCCN)NC1=O)=O)=O)(C)C)=O.[x]
Appearance

Solid

Color

White to off-white

Sequence

{D-Phe}-Cys-Tyr-{D-Trp}-{Orn}-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7)
Sequence Shortening

{D-Phe}-CY-{D-Trp}-{Orn}T{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (Need ultrasonic)

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL; Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.84%

SDS (252 KB)

COA (247 KB) LCMS (260 KB)

Handling Instructions (2659 KB)
References
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CTOP TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CTOPOpioid Receptorμ-opioid receptorKORpepideanalgesiaHypermotilityventral tegmental areaOpioidMu-opioid receptorNucleus accumbensLocomotor activityInhibitorinhibitorinhibit

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