Partial agonist
In pharmacology, a partial agonist is a substance that occupies a certain receptor ( lock and key principle ) and thereby partially imitates or replaces a transmitter (mediator) in its effect. In contrast to a (full) agonist, the partial agonist is only incompletely able to activate a receptor or the downstream signal transduction in the cell and to trigger an effect. Since a partial agonist is usually able to displace a (full) agonist from its receptor, a partial agonist can at least partially inhibit the effects of a (full) agonist. It therefore also has a "partially antagonistic" active component.
The development of partial agonists is of therapeutic interest in particular when the effect of an endogenous agonist is imitated, but its maximum effect is to be avoided, for example for safety reasons. An example of this is buprenorphine , which is used as a partial agonist at opioid receptors in pain therapy , but has a better safety profile compared to full agonists.
Individual evidence
- ↑ Dahan A, Yassen A, Romberg R, et al. : Buprenorphine induces ceiling in respiratory depression but not in analgesia . In: Br J Anaesth . 96, No. 5, May 2006, pp. 627-32. doi : 10.1093 / bja / ael051 . PMID 16547090 .