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.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
