CTAP TFA 

CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction^[1][2].

CTAP TFA (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect^[1].
CTAP TFA (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements^[1].
CTAP TFA 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 TFA is extensively protein-bound to albumin in the perfusion medium (68.2%) and to proteins in rat serum (84.2%)^[2].

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

1104.30 (free base)

C₅₁H₆₉N₁₃O₁₁S₂.xC₂HF₃O₂

固体

White to off-white

{d-Phe}-Cys-Tyr-{d-Trp}-Arg-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7)

{d-Phe}-CY-{d-Trp}-RT-{Pen}-T-NH2 (Disulfide bridge:Cys2-Pen7)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

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

• [1]. Mitchell J Bartlett, et al. Highly-selective µ-opioid Receptor Antagonism Does Not Block L-DOPA-induced Dyskinesia in a Rodent Model.BMC Res Notes  [Content Brief]

  [2]. Abbruscato TJ, et al. Blood-brain barrier permeability and bioavailability of a highly potent and mu-selective opioid receptor antagonist, CTAP: comparison with morphine. J Pharmacol Exp Ther. 1997 Jan;280(1):402-9.  [Content Brief]