How does GPCR work with opioid receptors and the antagonist Narcan?

Expert Solution

All Opioid receptor types located in Peripheral Nervous System, GI system, cerebral cortex, striatum, hippocampus, dorsal horn.

Types of opiods receptor:
mu receptors - midbrain periaqueductal gray
kappa receptors - midbrain periaqueductal gray
delta receptors - amygdala

How does GPCR (G-Protein coupled receptors) work with opioid receptors?

Answer:Opioids act by inhibiting GPCR that reduce activity in the cells that are associated with by reducing cAMP, increasing K+ flux, and decreasing Ca2+ influx.They also promote the release of endogenous opioids. like endorphins.

Pharmacological Effects associated with these receptor,

mu receptors: analgesia, sedation, miosis, euphoria, decreased respiration, constipation, pruritis.

kappa receptors: analgesia, sedation, miosis, dysphoria, micturition, diuresis, hallucinations.

delta receptors: analgesia, emotion/reward, seizures.

Narcan (Naloxone)

which is administered by injection.

Narcan (naloxone) are competitive opioid antagonists.They bind to opioid receptors without causing their activation.

Opioid receptors belong to the class A of G protein-coupled receptors (GPCR).

Narcan is act as a competitive antagonist at mc, κ, and σ opiate receptors in the CNS.also this drug has the highest affinity for the μ receptor.

Sydney Mullin answered 1 year ago

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