receptorcentered

Receptorcentered, also written as receptor-centered, is a descriptor used to denote a focus on receptor-level mechanisms as the primary determinants of pharmacological action. Rooted in receptor pharmacology, it emphasizes how ligand binding to specific receptor proteins, their affinity and intrinsic activity, receptor subtypes, and the associated signaling cascades shape physiological responses.

In drug discovery and research, a receptor-centered approach prioritizes characterizing ligand–receptor interactions, using assays for binding and functional responses, structure–activity relationships, and genetically modified models to delineate receptor roles. This perspective often informs lead optimization toward desired receptor profiles and functional selectivity.

The receptor-centered view coexists with, and is sometimes contrasted against, system-wide or network-based models that foreground downstream pathways, pharmacokinetics, and polypharmacology. Critics argue that overemphasizing receptor mechanisms may overlook emergent properties of complex biological systems or non-receptor targets.

Notable developments within this orientation include exploration of biased agonism, allosteric modulation, and receptor subtype selectivity across GPCRs and ion channels, illustrating how nuanced receptor signaling can yield distinct therapeutic effects with reduced side effects. Related terms include receptor pharmacology and pharmacodynamics.