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内源激动剂（如激素和神经递质）和外源（英语：exogenous）激动剂（如药物）都能激活受体。生理激动剂（英语：physiological agonism and antagonism）虽不与受体结合，但仍可产生相同生理反应。 内源性激动剂由身体自然产生，结合並激活特定受体，例如血清素作用于血清素受体，多巴胺作用于多巴胺受体。
PMID 17367094. Greasley PJ, Clapham JC; Clapham. Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge
drugs. Amsterdam: Slotervaart Hospital. （原始内容存档于2017-05-28） –通过U.S. Food and Drug Administration. Stewart MJ, Watson ID. Standard units for expressing
(AUC0–∞) and Total Amount Excreted (Ae∞) and Importance of Blood and Urine Sampling Scheme with Application to Digoxin.. Journal of Pharmacokinetics and Biopharmaceutics