6533b85afe1ef96bd12b9725
RESEARCH PRODUCT
Binding of several phenothiazine neuroleptics to a common binding site of alpha 1-acid glycoprotein, orosomucoid.
El-gamal SafaaWalter E. MüllerUwe Wollertsubject
Circular dichroismStereochemistryPharmaceutical ScienceOrosomucoidchemistry.chemical_compoundStructure-Activity RelationshipSingle sitePhenothiazinesPhenothiazinemedicineHumansBinding siteChlorpromazinechemistry.chemical_classificationBinding SitesbiologyChemistryCircular DichroismOrosomucoidBiochemistryα1 acid glycoproteinbiology.proteinGlycoproteinDialysismedicine.drugAntipsychotic AgentsProtein Bindingdescription
The interaction of several phenothiazine neuroleptics with alpha 1-acid glycoprotein was investigated using circular dichroism and equilibrium dialysis techniques. For chlorpromazine only, one high-affinity binding site of the protein was found. The binding of the drug to this single site generated typical polyphasic extrinsic Cotton effects. Since several other phenothiazine neuroleptics gave qualitatively comparable extrinsic Cotton effects in the presence of alpha 1-acid glycoprotein and potently inhibited the binding of chlorpromazine to the single site, it was concluded that all phenothiazine derivatives investigated bound preferentially to only one common binding site of the alpha 1-acid glycoprotein molecule.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1983-02-01 | Journal of pharmaceutical sciences |