Construct · 1 fields · 1 citations

inverse agonist: a standalone construct

One name. One construct. A landmark on the map.

● anchor · below-baseline receptor effect Nearest construct by meaning·not indexed
inverseagonist1 CONSTRUCTInverse agonistCOSTA & HERZ · 1989

A single standalone construct; nearby constructs are located against it in the Collider. Tap a field for its definition, unit, and measures.

Receptor pharmacology

A drug that pushes a receptor below its resting activity

An inverse agonist is a drug that binds a receptor with constitutive (baseline) activity and reduces that activity below its resting level, producing the opposite effect to an agonist rather than merely blocking one. Costa and Herz's 1989 work on delta opioid receptors demonstrated ligands with negative intrinsic activity, formalizing a third category beyond agonists and neutral antagonists. The referent is a drug that actively suppresses a receptor's spontaneous signalling, distinct from an antagonist that only prevents activation.[1]

Unit
The reduction in a receptor's constitutive activity produced by the drug
Recovery means
Not applicable
Measured by
Detected as a fall in basal receptor signalling in systems that show constitutive activity

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Nearby constructs

receptor2 fields · 2 citationsjingle · one word, two constructspartial agonist1 fields · 1 citationsanchor · submaximal receptor activationactivation4 fields · 4 citationsjingle · one word, four constructs

References

  1. Costa, T., & Herz, A. (1989). Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins. Proceedings of the National Academy of Sciences, 86(19), 7321–7325. https://doi.org/10.1073/pnas.86.19.7321

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