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PubMed1978

Interactions of narcotics and their antagonists with human serum esterase. VII: Further studies on the affinity of drugs for the substrate-binding site of the enzyme.

Earlier studies on the competitive inhibition of human serum esterase by morphine and related compounds were continued. Very good correlation was found between the inhibitor constants of 57 compounds and an empirical function, the "hydrophobic factor," which contains a positive contribution from the hydrophobic nature of a compound and negative contributions from its hydrophilic characteristics and from strain in its molecule. However, structural factors plainly also play a role in the affinity of each compound for the active site of the esterase because it was found necessary to include another positive term for a flexible hydrophobic group and because as a rule stereoisomers--even enantiomorphs--with identical hydrophobic factors differ in affinity; but no correlation could be found between the absolute configurations of the enantiomorphs and their affinities for the active site.

Binding Sites↗
PubMed1980

Interactions of narcotics and their antagonists with human serum esterase. VIII: structure-activity relationships of benzomorphans.

N-alkylbenzomorphans follow the pattern established in our earlier papers for the interaction of opiates with human serum esterase: they have affinity for both the substrate-binding site of the enzyme and an allosteric site at which agonistic drugs accelerate enzyme action. Affinity for the substrate-binding site is a function of the hydrophobicity of the drug, while affinity to the allosteric site is increased by alkyl groups at N and at C--5 and decreased by a 2'-methoxyl group or by either a methyl or a hydroxyl group in the 9 beta position. The absolute D configuration (corresponding to that of natural morphine) appears to be more sensitive to factors modifying affinity. All but three of the benzomorphans studied are agonists; all agonists have lower affinity for the allosteric site than antagonists.

Benzomorphans↗