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Selective Receptor Activation

Meaning

Selective Receptor Activation is a sophisticated pharmacological principle involving the use of therapeutic agents that are designed to bind and initiate a biological response only at a specific subtype of a hormone receptor, leaving other related receptor subtypes unaffected. This precision targeting allows clinicians to harness the beneficial effects of a hormone, such as testosterone or estrogen, in certain tissues while minimizing or eliminating undesirable side effects in other tissues. The clinical utility lies in achieving a highly localized and controlled therapeutic outcome, thereby improving the safety and efficacy profile of hormonal and peptide interventions. This approach is exemplified by the development of Selective Androgen Receptor Modulators (SARMs) or Selective Estrogen Receptor Modulators (SERMs).