Partial Agonist

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects - when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present.

Some currently common drugs that have been classed as partial agonists at particular receptors include: buspirone, aripiprazole, buprenorphine, and norclozapine.

Other articles related to "partial agonist, agonist":

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2-carboxamide potent and highly subtype-selective A-582941 partial agonist activates ERK1/2 and CREB phosphorylation enhances cognitive performance AR-R17779 full agonist, nootropic TC-1698 ...
Bretazenil
... to benzodiazepine binding sites where it acts as a partial agonist ... Its profile as a partial agonist and preclinical trial data suggests that it may have a reduced adverse effect profile ... from traditional 1,4 benzodiazepines by being a partial agonist and because it binds to alpha,1, 2, 3, 4, 5 and 6 subunit containing GABAA benzodiazepine receptor ...
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... Saralasin is a partial agonist of angiotensin II receptors, though It is commonly mistaken as a competitive antagonist ... Saralasin's distinction as a partial agonist is based on the fact that it's therapeutic effect (i.e ... II is pharmacodynamically similar to angiotensin II itself thus it is a partial agonist, because if it was an antagonist it would not elicit an effect when ...
agonists" class="article_title_2">5-HT2A Receptor - Ligands - Agonists - Partial Agonists
... used in treatment of migraine blocks 5-HT2A and 5-HT2C receptors, but sometimes acts as partial agonist, in some preparations ... The atypical antipsychotic aripiprazole is also a weak partial agonist ... OSU-6162 acts as a partial agonist at both 5-HT2A and dopamine D2 receptors (2S,6S)-2-(2,5-dimethoxy-4-bromobenzyl)-6-(2-methoxyphenyl)piperidine is a structurally constrained ...

Famous quotes containing the word partial:

    The one-eyed man will be King in the country of the blind only if he arrives there in full possession of his partial faculties—that is, providing he is perfectly aware of the precise nature of sight and does not confuse it with second sight ... nor with madness.
    Angela Carter (1940–1992)