Inverse agonist

In pharmacology, an inverse agonist is an agent which binds to the same receptor binding-site as an agonist for that receptor but exerts the opposite pharmacological effect. This is the case for certain types of receptors (e.g. certain histamine receptors / GABA receptors) which have intrinsic activity without the acting of a ligand upon them, which is also referred to as 'constitutive activity'.

Related Topics:
Pharmacology - Receptor - Agonist

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One particular example is R015-4513 which the inverse agonist of the benzodiazepine class of drugs (such as Xanax and Valium). R015-4513 and the benzodiazepines both utilize the same GABA binding site on neurons, yet R015-4513 has the opposite effect, producing severe anxiety rather than the sedative effect the benzodiazepines.

Related Topics:
R015-4513 - Benzodiazepine - Xanax - Valium - Benzodiazepines

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