| Bioactivity | 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]. | ||||||
| In Vivo | 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 (T1/2 > 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]. Animal Model: | ||||||
| Name | CTAP TFA | ||||||
| Sequence | Phe-Cys-Tyr-Trp-Arg-Thr-Pen-Thr-NH2 (Disulfide bridge:Cys2-Pen7) | ||||||
| Shortening | FCYWRT{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7) | ||||||
| Formula | C53H70F3N13O12S2 | ||||||
| Molar Mass | 1218.32 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | 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) |
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| Reference | [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 [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. |