C-8813 (thiobromadol) is a potent

μ-opioid receptor The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

with a distinctive chemical structure which is not closely related to other established families of opioid drugs. The ''trans''-isomer was found to be around 591 times more potent than

morphine Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...

in animal studies. The same study assigned a potency of 504 times that of morphine to the related compound BDPC. C-8813 is claimed to be similarly potent at the

δ-opioid receptor The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi alpha subunit, Gi/G0 and has enkephalins as it ...

, which antagonizes the μ-induced depression of breathing, presumably making the drug safer. C-8813 has never been approved for use in humans.

References

Arylcyclohexylamines Synthetic opioids Thiophenes Tertiary alcohols 4-Bromophenyl compounds Mu-opioid receptor agonists Delta-opioid receptor agonists {{analgesic-stub

See also

References