Cebranopadol

Short Summary : ORL-1 agonist

Category : Endocrinology and Hormones|Opioid Receptor

Purity : 0.98

CAS Number : 863513-91-1

Formula : C24H27FN2O

Molecular Weight : 378.48

SMILE : CN(C)C1(CCC2(CC1)C3=C(CCO2)C4=C(N3)C=CC(=C4)F)C5=CC=CC=C5

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist [1][2][3][4]. Nociceptin/orphanin FQ peptide (NOP) and opioid are available analgesics. They provide sufficient efficacy in many pain syndromes. However, they are not effective enough in neuropathic pain [1].Cebranopadol showed the highest receptor affinities at NOP and MOP of rat and human, while the affinity at KOP receptors was 3-38 fold lower affinity for KOP in the human and rat. Compare with NOP or MOP, affinity for DOP in humans is 20-fold lower [1][2].In model rats, Cebranopadol was antinociceptive after intravenous and oral administration.And its activity lasted longer (7 h) than that of same doses of fentanyl (30 min) and morphine (3 h). Also, intravenous cebranopadol was also useful in chronic pain models: the spinal nerve ligation model, bone cancer pain, painful diabetic neuropathy and complete Freund’s adjuvant (CFA)-induced arthritis [1].References:[1]. Sa at K, Jakubowska A, Kulig K. Cebranopadol: a first-in-class potent analgesic agent with agonistic activity at nociceptin/orphanin FQ and opioid receptors. Expert Opin Investig Drugs, 2015 , 12: 1-8. [2]. Lambert DG, Bird MF, Rowbotham DJ, et al. Cebranopadol: a first in-class example of a nociceptin/orphanin FQ receptor and opioid receptor agonist. Br J Anaesth, 2015, 114(3): 364-366.[3]. Schunk S, Linz K, Hinze C, et al. Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol. ACS Med Chem Lett, 2014, 5(8): 857-862. [4]. Linz K, Christoph T, Tzschentke TM, et al. Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. J Pharmacol Exp Ther, 2014, 349(3): 535-548.

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