Cebranopadol 是NOP 和 opioid receptor 激动剂，作用于人NOP，MOP，KOP 和δ-阿片肽(DOP)受体，K_i/EC₅₀ 分别为 0.9 nM/13 nM，0.7 nM/1.2 nM，2.6 nM/17 nM，18 nM/110 nM。

Cebranopadol is an analgesic NOP and opioid receptor agonist with K i s/EC 50 s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.

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EC50: 13±2 nM (hNOP receptor), 1.2±0.4 nM (hMOP receptor), 17±5 nM (hKOP receptor), 110±28 nM (hDOP receptor)

Cebranopadol binds with high affinity (subnanomolar to nanomolar range) to nociceptin/orphanin FQ peptide (NOP) and opioid receptors, with Ki of 1±0.5 nM, 2.4±1.2 nM, and 64±11 nM for rat NOP, mu-opioid peptide (MOP) receptor, and kappa-opioid peptide (KOP) receptor, and with Ki of 0.9±0.2 nM, 0.7±0.3 nM, and 2.6±1.4 nM for Rat NOP, MOP, and KOP receptor. has not independently confirmed the accuracy of these methods. They are for reference only.

Cebranopadol exhibits highly potent and efficacious antinociceptive and antihypersensitive effects in several rat models of acute and chronic pain (tail-flick, rheumatoid arthritis, bone cancer, spinal nerve ligation, diabetic neuropathy) with ED 50 values of 0.5-5.6 μg/kg after intravenous and 25.1 μg/kg after oral administration. In comparison with selective MOP receptor agonists, cebranopadol is more potent in models of chronic neuropathic than acute nociceptive pain. Cebranopadol’s duration of action is long (up to 7 hours after intravenous 12 μg/kg; >9 hours after oral 55 μg/kg in the rat tail-flick test). The antihypersensitive activity of cebranopadol in the spinal nerve ligation model is partially reversed by pretreatment with the selective NOP receptor antagonist J-113397 or the opioid receptor antagonist naloxone, indicating that both NOP and opioid rece

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[1]. Linz K, et al. Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. J Pharmacol Exp Ther. 2014 Jun;349(3):535-48.
[2]. de Guglielmo G, et al. Cebranopadol Blocks the Escalation of Cocaine Intake and Conditioned Reinstatement of Cocaine Seeking in Rats. J Pharmacol Exp Ther. 2017 Sep;362(3):378-384.

In Vitro: DMSO : 6.67 mg/mL (17.62 mM; Need ultrasonic)配制储备液