A model system for opiate-receptor interactions: Mechanism of opiate-cerebroside sulfate interaction

Tae Mook Cho, Jung Sook Cho, Horace H. Loh

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

Narcotic analgetics were shown to bind cerebroside sulfate (CS) with high affinity. The binding correlated well with their pharmacological potency. In order to understand opiate receptor interaction at the molecular level, we have proposed the use of CS as a model opiate receptor. In these studies, our data indicate that the binding of opiates is determined by the heptane solubility of the drugs and their affinity to CS. The affinity of the agonist to CS is higher than that of its corresponding antagonist. The difference in affinity between an agonist and its corresponding antagonist is mainly due to the strength of electrostatic bond formed between the protonated nitrogen of the drug and the sulfate group of CS. Furthermore, we have concluded that narcotic agonist-CS complexes are more hydrophobic (intimate ion pairs formation) while the antagonist-CS complexes are more hydrophilic (hydrated ion pairs) in nature.

Original languageEnglish (US)
Pages (from-to)231-244
Number of pages14
JournalLife Sciences
Volume18
Issue number2
DOIs
StatePublished - Jan 15 1976

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