Cebranopadol - CAS 863513-91-1
Catalog number: B0084-474871
Category: Inhibitor
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Molecular Formula:
C24H27FN2O
Molecular Weight:
378.491
COA:
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Targets:
Opioid Receptor
Description:
Cebranopadol is a novel first-in-class compound with potent agonist activity on opioid receptor like-1(ORL-1) and the well established mu opioid receptor. It showed antinociceptive and antihypertensive effects in a variety of different animal models of pain, suggesting its potential use for the treatment of chronic pain states.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474871 10 mg $198 In stock
B0084-474871 25 mg $398 In stock
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Purity:
>98%
Appearance:
Light Yellow to Yellow Solid
Synonyms:
GRT6005; 6-fluoro-N,N-dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine
Solubility:
Soluble to 10 mM in DMSO.
Storage:
Store at -20°C
MSDS:
Inquire
Boiling Point:
547.5±50.0 °C at 760 mmHg
Density:
1.23±0.1 g/cm3
InChIKey:
CSMVOZKEWSOFER-UHFFFAOYSA-N
InChI:
InChI=1S/C24H27FN2O/c1-27(2)23(17-6-4-3-5-7-17)11-13-24(14-12-23)22-19(10-15-28-24)20-16-18(25)8-9-21(20)26-22/h3-9,16,26H,10-15H2,1-2H3
Canonical SMILES:
CN(C)C1(CCC2(CC1)C3=C(CCO2)C4=C(N3)C=CC(=C4)F)C5=CC=CC=C5
Current Developer:
Grünenthal
1.Limited potential of cebranopadol to produce opioid-type physical dependence in rodents.
Tzschentke TM;Kögel BY;Frosch S;Linz K Addict Biol. 2017 Sep 25. doi: 10.1111/adb.12550. [Epub ahead of print]
Cebranopadol is a novel potent analgesic agonist at the nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors. As NOP receptor activation has been shown to reduce side effects related to the activation of μ-opioid peptide (MOP) receptors, the present study evaluated opioid-type physical dependence produced by cebranopadol in mice and rats. In a naloxone-precipitated withdrawal assay in mice, a regimen of seven escalating doses of cebranopadol over 2 days produced only very limited physical dependence as evidenced by very little withdrawal symptoms (jumping) even at cebranopadol doses clearly exceeding the analgesic dose range. In contrast, mice showed clear withdrawal symptoms when treated with morphine within the analgesic dose range. In the rat, spontaneous withdrawal (by cessation of drug treatment; in terms of weight loss and behavioral score) was studied after 4-week subacute administration. Naloxone-precipitated withdrawal (in terms of weight loss and behavioral score) was studied in the same groups of rats after 1-week re-administration following the spontaneous withdrawal period. In both tests, cebranopadol-treated rats showed only few signs of withdrawal, while withdrawal effects in rats treated with morphine were clearly evident.
2.Respiratory Effects of the Nociceptin/Orphanin FQ Peptide and Opioid Receptor Agonist, Cebranopadol, in Healthy Human Volunteers.
Dahan A;Boom M;Sarton E;Hay J;Groeneveld GJ;Neukirchen M;Bothmer J;Aarts L;Olofsen E Anesthesiology. 2017 Apr;126(4):697-707. doi: 10.1097/ALN.0000000000001529.
BACKGROUND: ;Cebranopadol is a novel strong analgesic that coactivates the nociceptin/orphanin FQ receptor and classical opioid receptors. There are indications that activation of the nociceptin/orphanin FQ receptor is related to ceiling in respiratory depression. In this phase 1 clinical trial, we performed a pharmacokinetic-pharmacodynamic study to quantify cebranopadol's respiratory effects.;METHODS: ;Twelve healthy male volunteers received 600 μg oral cebranopadol as a single dose. The following main endpoints were obtained at regular time intervals for 10 to 11 h after drug intake: ventilation at an elevated clamped end-tidal pressure of carbon dioxide, pain threshold and tolerance to a transcutaneous electrical stimulus train, and plasma cebranopadol concentrations. The data were analyzed using sigmoid Emax (respiration) and power (antinociception) models.;RESULTS: ;Cebranopadol displayed typical opioid-like effects including miosis, analgesia, and respiratory depression. The blood-effect-site equilibration half-life for respiratory depression and analgesia was 1.2 ± 0.4 h (median ± standard error of the estimate) and 8.1 ± 2.5 h, respectively. The effect-site concentration causing 50% respiratory depression was 62 ± 4 pg/ml; the effect-site concentration causing 25% increase in currents to obtain pain threshold and tolerance was 97 ± 29 pg/ml.
3.Antihyperalgesic, Antiallodynic, and Antinociceptive Effects of Cebranopadol, a Novel Potent Nociceptin/Orphanin FQ and Opioid Receptor Agonist, after Peripheral and Central Administration in Rodent Models of Neuropathic Pain.
Tzschentke TM;Linz K;Frosch S;Christoph T Pain Pract. 2017 Nov;17(8):1032-1041. doi: 10.1111/papr.12558. Epub 2017 Feb 25.
Cebranopadol is a novel and highly potent analgesic acting via nociceptin/orphanin FQ peptide (NOP) and opioid receptors. Since NOP and opioid receptors are expressed in the central nervous system as well as in the periphery, this study addressed the question of where cebranopadol exerts its effects in animal models of chronic neuropathic pain. Mechanical hypersensitivity in streptozotocin (STZ)-treated diabetic rats, cold allodynia in the chronic constriction injury (CCI) model in rats, and heat hyperalgesia and nociception in STZ-treated diabetic and control mice was determined after intraplantar (i.pl.), intracerebroventricular (i.c.v.), or intrathecal (i.th.) administration. In STZ-treated rats, cebranopadol (i.pl.) reduced mechanical hypersensitivity in the ipsilateral paw, but had no effect at the contralateral paw. In CCI rats, cebranopadol (i.pl.) showed antiallodynic activity at the ipsilateral paw. After administration to the contralateral paw, cebranopadol also showed ipsilateral antiallodynic activity, but with reduced potency and delayed onset. In diabetic mice, cebranopadol i.th. and i.c.v. decreased heat hyperalgesia with full efficacy and similar potency for both routes.
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