Binding of the tricyclic antidepressant imipramine (IMI) to neutral and negatively charged lipid membranes was investigated using a radioligand binding assay combined with centrifugation or filtration. Lipid bilayers were composed of brain phosphatidylcholine (PC) and phosphatidylserine (PS). IMI binding isotherms were measured up to IMI concentration of 0.5 mmol/l. Due to electrostatic attraction, binding between the positively charged IMI and the negatively charged surfaces of PS membranes was augmented compared to binding to neutral PC membranes. After correction for electrostatic effects by means of the Gouy-Chapman theory, the binding isotherms were described both by surface partition coefficients and by binding parameters (association constants and binding capacities). It was confirmed that binding of IMI to model membranes is strongly affected by negatively charged phospholipids and that the binding is heterogeneous; in fact, weak surface adsorption and incorporation of the drug into the hydrophobic core of lipid bilayer can be seen and characterized. These results support the hypothesis suggesting that the lipid part of biological membranes plays a role in the mechanism of antidepressant action.

• MeSH
• antidepresiva tricyklická analýza   chemie   MeSH
• centrifugace MeSH
• chemické modely * MeSH
• filtrace MeSH
• fosfatidylcholiny analýza   chemie   MeSH
• fosfatidylseriny analýza   chemie   MeSH
• fosfolipidy analýza   chemie   MeSH
• imipramin chemie   MeSH
• kinetika MeSH
• lipidové dvojvrstvy analýza   chemie   MeSH
• liposomy analýza   chemie   MeSH
• makromolekulární látky analýza   chemie   MeSH
• membrány umělé MeSH
• mozek metabolismus   MeSH
• radioligandová zkouška metody   MeSH
• skot MeSH
• vazebná místa MeSH
• zvířata MeSH
• Check Tag
• skot MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• hodnotící studie MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• antidepresiva tricyklická MeSH
• fosfatidylcholiny MeSH
• fosfatidylseriny MeSH
• fosfolipidy MeSH
• imipramin MeSH
• lipidové dvojvrstvy MeSH
• liposomy MeSH
• makromolekulární látky MeSH
• membrány umělé MeSH

• MeSH
• antidepresiva tricyklická analýza   MeSH
• lidé MeSH
• radioimunoanalýza metody   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• antidepresiva tricyklická MeSH