CTAP TFA 是一种强效、高选择性的、可透过血脑屏障的阿片受体 (μ opioid receptor) 拮抗剂，IC₅₀ 为 3.5 nM。CTAP TFA 对 δ opioid 受体 (IC₅₀=4500 nM) 和生长抑素受体 (somatostatin receptors) 具有超过 1200 倍的选择性。CTAP TFA 可用于L -多巴胺 (HY-N0304) 诱导的运动障碍 (LID) 和阿片类药物过量或成瘾的研究。

CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC 50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC 50 =4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.

Solid

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

CTAP TFA (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect.
CTAP TFA (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements.
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.
CTAP TFA is extensively protein-bound to albumin in the perfusion medium (68.2%) and to proteins in rat serum (84.2%). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

FCYWRT{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7)

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

[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.

In Vitro: H₂O : 100 mg/mL (82.08 mM; Need ultrasonic)配制储备液