| Identification | Back Directory | [Name]
CTOP | [CAS]
103429-31-8 | [Synonyms]
NTB
CTOP
NALTRIBEN
threoninamide
CYS2,TYR3,ORN5,PEN7-AMIDE
M.W. 1062.26 C50H67N11O11S2
(Tyr3,Orn5,Pen7)-Octreotate amide
Cys2, Tyr3, Orn5, Pen7 amide - CTOP
DPHE-CYS-TYR-DTRP-ORN-THR-PEN-THR-OL
D-PHE-CYS-TYR-D-TRP-ORN-THR-PEN-THR-NH2
CTOP, (Tyr3,Orn5,Pen7)-Octreotate aMide
D-PHE-CYS-TYR-D-TRP-ORN-THR-PEN-THR AMIDE
H-D-PHE-CYS-TYR-D-TRP-ORN-THR-PEN-THR-NH2
FCYW(ORN)T(PEN)T-NH2 (DISULFIDE BRIDGE: 2-7)
[Cys2, Tyr3, Orn5, Pen7-amide]-Somatostatin 14 (7-14)
[CYS2, TYR3, ORN5, PEN7]-SOMATOSTATIN 14 (7-14), AMIDE
D-Phe-L-Cys(1)-L-Tyr-D-Trp-L-Orn-L-Thr-L-Pen(1)-L-Thr-NH2
H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (Disulfide bond)
H-D-PHE-CYS-TYR-D-TRP-ORN-THR-PEN-THR-NH2 (DISULFIDE BRIDGE: 2-7)
D-Phe-L-Cys(1)-L-Tyr-D-Trp-L-Orn-L-Thr-3-Mercapto(1)-L-Val-L-Thr-NH2
phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)
H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2, (Disulfide bond between Cys2 and Pen7)
phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide
L-Threoninamide, D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-ornithyl-L-threonyl-3-mercapto-L-valyl-, cyclic (2→7)-disulfide | [Molecular Formula]
C50H67N11O11S2 | [MDL Number]
MFCD00076708 | [MOL File]
103429-31-8.mol | [Molecular Weight]
1062.26 |
| Chemical Properties | Back Directory | [Boiling point ]
1491.2±65.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [RTECS ]
XO8578200 | [storage temp. ]
-20°C | [form ]
Powder | [pka]
9.90±0.15(Predicted) | [color ]
white | [Water Solubility ]
Soluble to 1 mg/ml in water | [Sequence]
{D-Phe}-Cys-Tyr-{D-Trp}-{Orn}-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7) |
| Hazard Information | Back Directory | [Uses]
CTOP has been used:
- to study the anxiogenic effects induced by CTOP in mice and rat.
- to study the effect of μ-opioid antagonist, CTOP on the bovine milk-derived LF (BLF)-induced analgesia.
- to determine whether μ-opioid receptors act cooperatively with 5-hydroxytryptamine (5-HT1A) receptors to regulate the behaviors generated in the elevated T-maze (ETM).
| [Uses]
CTOP is a μ-opioid receptor antagonist which has been shown to regulate behaviour and expression in rats. An endogenous opioid peptide which may also be used in the treatment of pain through improved morphine tolerance via blocking of mTOR. | [General Description]
D-Pen-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) is a selective cyclic μ-opioid receptor antagonist. | [Biochem/physiol Actions]
Selective ligand for μ-opioid receptors. | [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. |
| [IC 50]
μ Opioid Receptor/MOR | [storage]
Store at -20°C |
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