The Sound of Evolution
Oxymorphone
Mechanism of action:
Oxymorphone is an opioid and a semi-synthetic morphinan derivative. Oxymorphone primarily acts on mu-opioid receptors. Through Gi/o protein coupling, it inhibits adenylate cyclase, reduces cAMP production, suppresses presynaptic voltage-gated Ca2+ channels, blocks calcium influx, and decreases the release of pain-related neurotransmitters such as glutamate and substance P. At the same time, it activates postsynaptic K+ channels, promotes potassium efflux, and causes neuronal hyperpolarization.
Reference(s):
1. Spetea M et al. (1998). Affinity profiles of novel delta-receptor selective benzofuran derivatives of non-peptide opioids. Neurochem Res.
2. Lemberg KK et al. (2006). Antinociception by spinal and systemic oxycodone: why does the route make a difference? In vitro and in vivo studies in rats. Anesthesiology.