PZM21

PZM21 is a novel synthetic opioid drug that was discovered in 2016 through structure-based drug design. It is a G protein-biased agonist of the μ-opioid receptor, which is the main target of most opioid drugs. PZM21 is unique in that it does not recruit β-arrestin-2, a protein that is thought to be responsible for many of the side effects of traditional opioids. This makes PZM21 a promising candidate for the development of safer opioid drugs.

Discovery

PZM21 was discovered by a team of researchers at Stanford University and the University of California, San Francisco. The team used a computational approach to design the drug, which involved screening over three million compounds to find those that would bind to the μ-opioid receptor in a specific way. The result was a compound that is structurally distinct from all known opioids and has unique pharmacological properties.

Pharmacology

PZM21 is a G protein-biased agonist of the μ-opioid receptor. This means that it preferentially activates the G protein signaling pathway over the β-arrestin-2 pathway. Most opioids activate both pathways, but the β-arrestin-2 pathway is thought to be responsible for many of the side effects of these drugs, including respiratory depression, constipation, and addiction. By avoiding this pathway, PZM21 may be able to produce analgesic effects with fewer side effects.

Potential Applications

The unique pharmacology of PZM21 makes it a promising candidate for the development of safer opioid drugs. However, more research is needed to fully understand its effects and potential applications. As of 2016, PZM21 has only been tested in mice, and it is not yet clear whether its beneficial effects will translate to humans.

See Also

• Opioid
• μ-opioid receptor
• G protein
• β-arrestin-2

PZM21

• 
•