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编 号:F015199
分子式:C51H69N13O11S2
分子量:1104.3
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生物活性:
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.

体内研究:
CTAP (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect.CTAP (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements.CTAP is stable in the blood and serum of rats (T1/2 > 500 min), showing that the structure of this peptide offers enzymatic resistance. CTAP is extensively protein-bound to albumin in the perfusion medium (68.2%) and to proteins in rat serum (84.2%).Animal Model:Male Sprague-Dawley rats
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.
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