Dose response curves of a full agonist, partial agonist, neutral antagonist, and inverse agonist. In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.

2024年10月16日 · What is Inverse agonist? Inverse agonist is a molecule or chemical compound that can bind to the same receptor site as an agonist and produces a biological response opposite to that of the agonist i.e. exhibits negative efficacy. For example, Flumazenil produces an anxiogenic effect at the GABA (Gamma-Aminobutyric Acid) receptor.

反向激动剂（英語： inverse agonist ）在药理学中是指和激动剂结合在相同的受体上，但引起相反的药理反应的物质。根据定义，反向激动剂的效能为负。 能受反向激动剂作用的受体在没有结合任何配体必须有内在的基础活性。激动剂能增加其活性，而反向激动剂 ...

An inverse agonist, also known as a negative antagonist, is a type of ligand that exhibits negative efficacy. It is suggested that the nomenclature of inverse agonism should be expanded to include ligands that act at ectopic sites on receptors, reflecting the underlying topology of interaction.

Using the inverse agonist, SB 206553, Navailles et al (2006) demonstrated that constitutive activity of the serotonin type 2C receptor differed between the nucleus accumbens and the ventral tegmental area. Consequently, a drug with inverse agonist properties may behave as a strong inverse agonist, a weak inverse agonist, and as an antagonist in ...

The inverse agonist mechanism-of-action of the atypical antipsychotic drugs showed greater inverse agonism at the 5HT 7 receptors as compared to typical agents. An important implication of inverse agonism at serotonin receptors is development of compounds which have antipsychotic and antiparkinsonian activities.

Inverse agonists are compounds that interact with receptor-signal transduction systems that have a constitutive level of activity, and through interaction with the receptor, reduce the activity in the direction opposite of that of a pure agonist.

Nearly all H(1) and H(2) antihistaminics (antagonists) have been shown to be inverse agonists. Among the β-blockers, carvedilol and bucindolol demonstrate low level of inverse agonism as compared to propranolol and nadolol.

In the inverse agonist two state model, inverse agonists bind with the constitutively active receptors, stabilize them and shifts receptor equilibrium towards the inactive state, reducing the level of basal activity ie: negative efficacy or negative intrinsic activity. Here is the integrated view :

Inverse agonist is a ligand that binds to the same receptor-binding site as an agonist and not only antagonizes the effects of an agonist but, moreover, exerts the opposite effect by suppressing spontaneous receptor signaling (when present).