Partialagonist

A partial agonist is in pharmacology, a substance that a certain receptor occupied ( key - lock principle ), while a transmitter ( mediator) in its effect mimics partially, or replaced. The partial agonist, in contrast to a (full) agonists incomplete able to activate a receptor or downstream signal transduction in the cell and trigger an effect. As a partial agonist is usually able to eliminate a (full) agonist from its receptor, a partial agonist may be at least partially inhibit the effects of a (full) agonists. Thus He also has a " partialantagonistische " active component.

The development of partial agonist is particularly therapeutic interest, if the effect of a body's own ( endogenous ) agonists mimics, but to achieve the maximum effect, for example for safety reasons, should be avoided. An example of this is buprenorphine, which is used as a partial agonist of opioid receptors in pain, but compared to full agonist has a better safety profile.

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