What is partial agonist?

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.

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Some articles on partial agonist:

Saralasin
... 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 ... similar to angiotensin II itself thus it is a partial agonist, because if it was an antagonist it would not elicit an effect when bound to it's receptor ...
Alpha-7 Nicotinic Receptor - Ligands - Agonists
... 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 subtype-selective neuroprotective ...
5-HT2A Receptor - Ligands - Agonists - Partial Agonists
5-HT2A and 5-HT2C receptors, but sometimes acts as partial agonist, in some preparations ... 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 ...
Bretazenil
... due to its high affinity binding 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 ... Bretazenil differs 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 complexes ...
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 ... 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 ... 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 ...

Famous quotes containing the word partial:

    America is hard to see.
    Less partial witnesses than he
    In book on book have testified
    They could not see it from outside....
    Robert Frost (1874–1963)