ChemicalBook CAS DataBase List 103429-32-9

103429-32-9

Name	CTAP
CAS	103429-32-9
Molecular Formula	C51H69N13O11S2
MDL Number	MFCD00671434
Molecular Weight	1104.3
MOL File	103429-32-9.mol

Synonyms

CTAP CTAP-NH2 CTAP,CTA CTAP, ≥95% 7)-disulfide CYS2, TYR3, ARG5, PEN7-AMIDE M.W. 1104.30 C51H69N13O11S2 D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2 H-D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2 D-Phe-L-Cys-L-Tyr-D-Trp-L-Arg-L-Thr-L-Pen-L-Thr-NH2 H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(Cys2-Pen7) D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2(DISULFIDE BRIDGE:CYS2-PEN7) H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (Disulfide bond between Cys2 and Pen7) L-Threoninamide,D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-arginyl-L-threonyl-3-mercapto-L-valyl-,cyclic (2&reg D-Phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-arginyl-L-threonyl-3-mercapto-L-valyl-L-threoninamide cyclic (2&#8594 D-Phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-arginyl-L-threonyl-3-mercapto-L-valyl-L-threoninamide cyclic (2-7)-disulfide L-Threoninamide, D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-arginyl-L-threonyl-3-mercapto-L-valyl-, cyclic (2→7)-disulfide

Chemical Properties

storage temp.	-20°C
form	Solid
color	off-white
Water Solubility	Soluble to 1 mg/ml in water
Sequence	{d-Phe}-Cys-Tyr-{d-Trp}-Arg-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7)

Safety Data

WGK Germany

Hazard Information

Uses

CTAP acts as a selective μ-opioid receptor antagonist with a multitude of applications including the regulation of aggressive behavior in mammals. Activation of μ-opioid receptors in the central nucleus of the amygdala, is responsible for mechanisms related to the control of sodium appetite and regulation of sodium intake.

Uses

CTAP has been used as a μ-opioid receptor (MOR) antagonist:

to study the anti-hyperalgesic effect of dipeptidyl peptidase 4 (DPP4) inhibitor isoleucine-proline-isoleucine (IPI) and vildagliptin in carrageenan-induced inflammation
to study the role of MOR in glutamate and gamma-aminobutyric acid (GABA) efflux during predator stress in rats
to determine the endogenous opioid peptide involved in blocking pain induced by activated gastrin-releasing peptide (Grp⁺) neurons

Biochem/physiol Actions

CTAP is a peptide antagonist produced from somatostatin analogs.

in vivo

CTAP (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect^[1].
CTAP (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements^[1].
CTAP is stable in the blood and serum of rats (T_1/2 > 500 min), showing that the structure of this peptide offers enzymatic resistance^[2].
CTAP is extensively protein-bound to albumin in the perfusion medium (68.2%) and to proteins in rat serum (84.2%)^[2].

Animal Model:	Male Sprague-Dawley rats^[1]
Dosage:	0, 0.1, 0.5, 1 mg/kg
Administration:	IP, single
Result:	Completely blocked morphine’s antinociceptive effect at 0.5 or 1 mg/kg.

IC 50

μ Opioid Receptor/MOR: 3.5 nM (IC₅₀); δ Opioid Receptor/DOR: 4500 nM (IC₅₀)

storage

Desiccate at -20°C

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