First-pass extracted concept

inverse agonism

Candidate: concept label1 source documents4 linked claims

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Evidence Snippets

This phenomenon has been termed inverse agonism and the corresponding ligands are referred to as inverse agonists.

Evidence 1Source 1DOI PubMedprovenance

Supporting Sources

Source 1review2000British Journal of PharmacologyDOI PubMed

1 evidence snippet 4 linked claims Claim 1 Claim 2 Claim 3

Linked Claims

Claim 1limitationsupports2000Source 1DOI PubMed

Classification of ligands as inverse agonists, neutral antagonists, or partial agonists is strongly dependent on receptor system and experimental conditions.

Claim 2mechanistic modelsupports2000Source 1DOI PubMed

GPCRs can display constitutive activity in the absence of agonist, and some ligands previously considered antagonists can suppress this spontaneous activity as inverse agonists with negative intrinsic activity.

Claim 3mechanistic modelsupports2000Source 1DOI PubMed

The concept of inverse agonism supports a two-state GPCR model in which receptors pre-exist in equilibrium between active and inactive states.

Claim 4translational relevancemixed2000Source 1DOI PubMed

Inverse agonism and constitutive receptor activity are unequivocally demonstrated in vitro, but their pathophysiological consequences remain far from self-evident.