allosteric modulation
Pronunciation: al-oh-STER-ik mod-yoo-LAY-shun
Indirect drug action where compounds bind to sites other than the primary receptor binding site to alter receptor function.
Full Definition
Allosteric modulation refers to a mechanism of drug action where therapeutic compounds bind to allosteric sites (locations distinct from the orthosteric or primary binding site) on neurotransmitter receptors or enzymes. This binding can either enhance (positive allosteric modulation) or inhibit (negative allosteric modulation) the receptor's response to its natural ligand. In psychopharmacology, allosteric modulators are increasingly important as they can provide more nuanced therapeutic effects with potentially fewer side effects compared to direct receptor agonists or antagonists. Examples include certain GABA receptor modulators and glutamate receptor modulators used in psychiatric treatment.
Usage
Usage note: Often abbreviated as PAM (positive allosteric modulation) or NAM (negative allosteric modulation) in clinical literature.
In Context
- "The novel anxiolytic works through positive allosteric modulation of GABA-A receptors rather than direct benzodiazepine site binding." — Research publication
- "Allosteric modulation allows for more selective therapeutic effects while preserving physiological receptor function." — Clinical review article