Naloxonazine

Naloxonazine is a derivative of Naloxone, a medication used to counter the effects of opioid overdose. Naloxonazine is a selective mu-opioid receptor antagonist, which means it blocks the action of opioids at the mu-opioid receptor in the brain and nervous system.

Chemistry

Naloxonazine is a morphinan derivative, which is a class of chemicals that includes many opioids and opioid antagonists. It is structurally similar to naloxone, but has a methylene bridge connecting the two nitrogen atoms in the morphinan ring system. This modification increases its selectivity for the mu-opioid receptor.

Pharmacology

Naloxonazine acts as an irreversible antagonist at the mu-opioid receptor. This means that once it binds to the receptor, it does not unbind, effectively blocking the receptor for a prolonged period of time. This is in contrast to naloxone, which is a reversible antagonist and can be displaced from the receptor by a sufficiently high concentration of an opioid.

Clinical Use

While naloxonazine is not used clinically, it is a valuable tool in research. It is used to study the role of the mu-opioid receptor in pain, addiction, and other neurological processes. Its irreversible binding allows for long-term studies of receptor function.

See Also

• Naloxone
• Opioid receptor
• Opioid overdose

References

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