Inverse agonist

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Inverse Agonist

Inverse agonist (pronunciation: /ɪnˈvɜːrs ˈæɡənɪst/) is a type of ligand that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.

Etymology

The term "inverse agonist" originates from the Latin inversus, meaning "turned inside out", and the Greek ἀγωνιστής (agonistēs), meaning "combatant, champion". It was first used in the field of pharmacology in the late 20th century.

Function

An inverse agonist can reduce the activity of a receptor below its baseline level, as opposed to an antagonist, which merely blocks the activity of the agonist. This is achieved by stabilizing the inactive form of the receptor, thereby decreasing the likelihood of the receptor transitioning to its active state.

Examples

Examples of inverse agonists include Naloxone and Naltrexone, which are used to treat opioid overdoses and addiction, respectively. These drugs bind to opioid receptors in the brain and reduce their activity, thereby counteracting the effects of opioids.

Related Terms

  • Agonist: A molecule that activates a receptor to produce a biological response.
  • Antagonist: A molecule that prevents the action of an agonist without having any effect itself.
  • Ligand: A molecule that binds to a receptor.
  • Receptor: A protein molecule that receives chemical signals from outside a cell.

External links

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