JNJ 20788560 - CAS 825649-28-3
Catalog number: 825649-28-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Opioid Receptor
JNJ-20788560 is a delta opioid agonist analgesics. No recent reports of development identified for preclinical development in Inflammatory-pain in USA.
JNJ-20788560; JNJ 20788560; JNJ20788560; 9-(8-Azabicyclo(3.2.1)oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide
Soluble in DMSO
-20℃ Freezer
Inflammatory pain; Pain
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Janssen Research & Development
1.JNJ-20788560 [9-(8-azabicyclo[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide], a selective delta opioid receptor agonist, is a potent and efficacious antihyperalgesic agent that doe
Codd EE1, Carson JR, Colburn RW, Stone DJ, Van Besien CR, Zhang SP, Wade PR, Gallantine EL, Meert TF, Molino L, Pullan S, Razler CM, Dax SL, Flores CM. J Pharmacol Exp Ther. 2009 Apr;329(1):241-51. doi: 10.1124/jpet.108.146969. Epub 2009 Jan 16.
Mu-opioid analgesics are a mainstay in the treatment of acute and chronic pain of multiple origins, but their side effects, such as constipation, respiratory depression, and abuse liability, adversely affect patients. The recent demonstration of the up-regulation and membrane targeting of the delta-opioid receptor (DOR) following inflammation and the consequent enhanced therapeutic effect of delta-opioid agonists have enlivened the search for delta-opioid analgesic agents. JNJ-20788560 [9-(8-azabicyclo-[3.2.1]oct-3-ylidene)-9H-xanthene-3-carboxylic acid diethylamide] had an affinity of 2.0 nM for DOR (rat brain cortex binding assay) and a naltrindole sensitive DOR potency of 5.6 nM (5'-O-(3-[(35)S]thio)triphosphate assay). The compound had a potency of 7.6 mg/kg p.o. in a rat zymosan radiant heat test and of 13.5 mg/kg p.o. in a rat Complete Freund's adjuvant RH test but was virtually inactive in an uninflamed radiant heat test. In limited studies, tolerance was not observed to the antihyperalgesic or antinociceptive effects of the compound.
2.Ex vivo delta opioid receptor autoradiography: CNS receptor occupancy of two novel compounds over their antihyperalgesic dose range.
Codd EE1, Ma J, Zhang SP, Stone DJ Jr, Colburn RW, Brandt MR, Chevalier KM, Zhu Y, Peng S, Cai C, Acton PD, Flores CM. Pharmacol Biochem Behav. 2010 Aug;96(2):130-5. doi: 10.1016/j.pbb.2010.04.020. Epub 2010 May 12.
Discovered as part of an effort to identify delta opioid (DOPr or DOR) agonist analgesics, JNJ-20788560 and JNJ-39204880 exhibited high DOR affinity, with K(i) values of 1.7 and 2.0nM, respectively, and were selective for DOR over the mu opioid receptor (MOPr or MOR), with 596- and 122-fold selectivity, respectively. Both compounds stimulated DOR but not MOR induced GTPgammaS binding and were effective antihyperalgesic agents in the complete Freund's adjuvant model of thermal hyperalgesia in the rat, with oral ED(50) values of 13.5 and 35mg/kg, corresponding to plasma levels of 1 and 9microM, respectively. Autoradiographic analysis of DOR and MOR occupancy in sections of brain (striatum) and lumbar spinal cord (L4-L6) was determined ex vivo, using radiolabeled naltrindole or DAMGO. Quantitative image analysis resulted in striatal DOR ED(50) values of 6.9 and 10.7mg/kg, for JNJ-20788560 and JNJ-39204880 respectively, and spinal cord values of 6.
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CAS 825649-28-3 JNJ 20788560

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