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- W2051213573 abstract "After alkylation of a fraction of the total α-adrenoreceptors by phenoxybenzamine in rat vas deferens, the dissociation constants of (−)- and (+)-epinephrine in functional studies were 7 × 10−7 M and 2 × 10−5 M, respectively. In the adrenoreceptor-containing tissue fraction, when 3H-labeled WB4101 was used as the interacting ligand, for each enantiomer who affinity sites were found. Only the low-affinity dissociation consant for each isomer correlates with the constant obtained from the functional studies. If the change in Gibb's free energy. ΔG°, is calculated from the low-affinity binding constants, the values −8.1 and −6.2 kcal/mol for (−)- and (+)-isomer, respectively, are obained. The small difference in the value between isomers forms a hydrogen bond with the receptor. The interaction of epinephrine with this receptor appears to be driven largely by the entropy of the drug-receptor interaction with only a small nonsteroselective contribution from the enthalpy of ineraction." @default.
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- W2051213573 date "1989-01-01" @default.
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- W2051213573 title "Pharmacologic implications of ?-adrenocreceptor interactive parameters for epinephrine enantiomers in the rat vas deferens" @default.
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- W2051213573 doi "https://doi.org/10.1002/chir.530010106" @default.
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