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

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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 9 months ago

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