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CLARK (1926), KOSHLAND, ARIËNS (1954), STEPHENSON (1956), LEFF,…
CLARK (1926)
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Action of the drug = f (fixation, ability to elicit the response)
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KOSHLAND
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2) Drug (D) approaches the receptor --> conformational change on the receptor (Ra to Rb). Rb shows the bonding site to the drug
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ARIËNS (1954)
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Action of the drug = f (affinity, intrinsic activity (alpha))
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LEFF, SCARAMANELLINI, et al.
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CLARK & ARIÉNS
consider that there was a linear relationship between the nº of occupied receptors and the BR (kd = E50)
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FURCHGOTT (1966)
efficacy (not only depends on the drug) = f(tissue, nº of receptors on that tissue, receptors reserve...)
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