Inverse agonist

As an inverse agonist substances are referred to in pharmacology, which bind to a spontaneously active receptor and reduce its activity. An inverse agonist therefore resulting in contrast to an agonist to a negative effect.

Occasionally, the inverse agonist be counted among the antagonists. Just occasionally imprecise negative allosteric modulators are referred to as inverse agonists.

In theory, an inverse agonism at all receptors are observed to show the spontaneous activity ( constitutive activity). For example, antihistamines inhibit the spontaneously active histamine receptors H1, ​​H2 and H3 and are used inter alia as antiallergic agents. Further targets for the development of an inverse agonist, for example, beta -adrenoceptors, dopamine receptors D2 and D3, the serotonin receptor 5-HT1A, 5 - HT1B, 5 -HT2C and 5 -HT7, the formyl peptide receptor, VIP receptor, and the viral chemokine receptor US28 which have also under physiological conditions, spontaneous activity or as a result of pathological changes show (eg mutation or overexpression ).