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Encyclopedia > 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'. Pharmacology (in Greek: pharmacon (φάρμακον) is drug, and logos (λόγος) is science) is the study of how chemical substances interact with living systems. ... Receptor may refer to: In telecommunication, a receiver. ... Agonists An agonist is a substance that binds to a receptor and triggers a response by the cell. ...


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. Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ... Alprazolam, is an anxiolytic benzodiazepine used to treat anxiety disorders. ... Diazepam, brand names: Valium, Seduxen, in Europe Apozepam, is a 1,4-benzodiazepine derivative, which possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ...


  Results from FactBites:
 
About Inverse Agonists (720 words)
In the absence of agonist, this conformation is scarce.
Addition of the inverse agonist stabilizes the inactive conformation of the receptor and drives the equilibrium away from the active conformation.
Inverse agonists probably bind to and stabilize the inactive form, which pushes the equilibrium away from the spontaneous formation of the active conformation of the receptor.
Inverse agonist - Wikipedia, the free encyclopedia (298 words)
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.
The pharmacological effect of an inverse agonist is measured as the negative value of the agonist primarily due to the historical findings of the already known agonist.
One particular example is R015-4513 which is the inverse agonist of the benzodiazepine class of drugs (such as Xanax and Valium).
  More results at FactBites »

 

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