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Receptor Antagonism

Meaning

Receptor antagonism is a pharmacological mechanism where a substance, known as an antagonist, binds to a specific cellular receptor without activating it, thereby blocking the binding and subsequent biological effect of the natural or endogenous hormone or neurotransmitter. This action effectively prevents the intended cellular signaling pathway from being initiated. Clinically, receptor antagonists are used to counteract the effects of overactive hormones or to mitigate the side effects of other therapeutic agents. This principle is a cornerstone of modern endocrinology and drug development.