| Bioactivity | CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction[1][2]. |
| 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 (T1/2 > 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: |
| Name | CTAP |
| CAS | 103429-32-9 |
| Sequence | {d-Phe}-Cys-Tyr-{d-Trp}-Arg-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7) |
| Shortening | {d-Phe}-CY-{d-Trp}-RT-{Pen}-T-NH2 (Disulfide bridge:Cys2-Pen7) |
| Formula | C51H69N13O11S2 |
| Molar Mass | 1104.30 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |