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Cebranopadol

CAS No. : 863513-91-1

MCE 国际站：Cebranopadol

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: Cebranopadol binds with high affinity (subnanomolar to nanomolar range) to nociceptin/orphanin FQ peptide (NOP) and opioid receptors, with K_i 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 K_i of 0.9±0.2 nM, 0.7±0.3 nM, and 2.6±1.4 nM for Rat NOP, MOP, and KOP receptor.

In Vivo: 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 ED₅₀ 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 receptor agonism are involved in this activity.

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