Surface pharmacology: Drug binding equilibria and ion transport in membrane structures

Blank, Martin

doi:10.1016/0163-7258(79)90034-2

Cited by 7 publications

(3 citation statements)

References 28 publications

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“…The conditions for its applicability are not likely to be fulfilled in the usual complex physicochemical receptor−ligand interaction, say in a membrane or protein. In such systems “surface phenomena” pointed out by Blank are likely to occur. The term surface phenomena should here be regarded as a vague description of the complex interaction of ligands with the binding sites on the surface of a membrane, or within the membrane interior, or on a macromolecule.…”

Section: The δS° > 0 Binding Mechanismmentioning

confidence: 99%

Entropic Trapping Binding Mechanism: Its Likely Role in Receptor−Ligand and Other Biochemical Systems

Miklavc

Kocjan

2004

J. Chem. Inf. Comput. Sci.

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Entropy-driven binding continues to be discovered in receptor-ligand systems as well as in other important biochemical systems. In receptor-ligand systems the "thermodynamic agonist-antagonist discrimination" is often found: in some such receptor types the binding of antagonists is entropy-driven, in others this is a characteristic of the agonist binding. The interpretation of the entropy-driven binding mechanism in the systems in question is still rather elusive. Experimental findings clearly indicate that the entropic binding mechanisms which are usually considered cannot provide a consistent interpretation in these cases. Entropic trapping was therefore proposed in our earlier papers as a possible binding model which does not contradict the experimental facts. It is pointed out here that through the work which has appeared subsequently the existence of such a mechanism has been firmly established and that its role is strongly corroborated by the more recent data from several biochemical systems.

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Section: The δS° > 0 Binding Mechanismmentioning

confidence: 99%

Entropic Trapping Binding Mechanism: Its Likely Role in Receptor−Ligand and Other Biochemical Systems

Miklavc

Kocjan

2004

J. Chem. Inf. Comput. Sci.

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“…These conditions are certainly not fulfilled in the present kind of ligand-receptor binding studies, where we are dealing with interactions between ligands of complex physicochemical nature and sites on nonsolubilized membranes. For such systems, surface phenomena, of which the importance for pharmacology was recently put forward by Blank (1979), are likely to occur.…”

Section: Role Of Physicochemical Properties and Surface Phenomena In mentioning

confidence: 99%

“…Finally, anomalous equilibrium binding patterns are discussed in relation to the physicochemical properties of catechol dopamine agonists and dopamine antagonists. The important, but often ignored, fact of the occurrence of surface phenomena on membranes is considered (Blank, 1979).…”

mentioning

confidence: 99%

Optimal Conditions for [³H]Apomorphine Binding and Anomalous Equilibrium Binding of [³H]Apomorphine and [³H]Spiperone to Rat Striatal Membranes: Involvement of Surface Phenomena Versus Multiple Binding Sites

Leysen

Gommeren

1981

Journal of Neurochemistry

127

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I. Binding of [3H] apomorphine to dopaminergic receptors in rat striatum was most reproducible and clearly detectable when incubations were run at 25 degrees C in Tris-HCl buffer, pH 7.5, containing 1 mM-EDTA and 0.01% ascorbic acid, using a washed total-membrane fraction. The receptor binding was stereospecifically inhibited by (+)-butaclamol, and dopamine agonists and antagonists showed high binding affinity for these sites. Unlabelled apomorphine inhibited an additional nonstereospecific binding site, which was unrelated to dopamine receptors. EDTA in the incubation mixture considerably lowered nonstereospecific [3H]apomorphine binding, apparently by preventing the complexation of the catechol moiety with metal ions which were demonstrated in membrane preparations. Stereospecific [3H]apomorphine binding was not detectable in the frontal cortex, whereas in the absence of EDTA much saturable nonstereospecific binding occurred. II. Kinetic patterns of stereospecific [3H]spiperone and [3H]apomorphine binding to rat striatal membranes and the inhibition patterns of a dopamine antagonist and an agonist were evaluated at different temperatures in high-ionic-strength Tris buffer with salts added and low-ionic-strength Tris buffer with EDTA. Apparent KD values of spiperone decreased with decreasing tissue concentrations. KD values of both spiperone and apomorphine were little influenced by temperature changes. Scatchard plots of the stereospecific binding changed from linear to curved; the amount of nonstereospecific binding of the 3H ligands varied considerably, but in opposite directions for spiperone and apomorphine in the different buffers. In various assay conditions, interactions between agonists, and between antagonists, appeared fully competitive, but agonist-antagonist interactions were of mixed type. The anomalous binding patterns are interpreted in terms of surface phenomena occurring upon reactions of a ligand with complex physicochemical properties and nonsolubilized sites on membranes suspended in a buffered aqueous solution. It is concluded that anomalous binding patterns are not necessarily an indication of binding to multiple sites or involvement of distinct receptors for high-affinity agonist and antagonist binding.

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Transmembrane Potential and Redox Reactions from a Physiological Point of View

Blank

1983

Bioelectrochemistry I

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Surface pharmacology: Drug binding equilibria and ion transport in membrane structures

Cited by 7 publications

References 28 publications

Entropic Trapping Binding Mechanism: Its Likely Role in Receptor−Ligand and Other Biochemical Systems

Entropic Trapping Binding Mechanism: Its Likely Role in Receptor−Ligand and Other Biochemical Systems

Optimal Conditions for [³H]Apomorphine Binding and Anomalous Equilibrium Binding of [³H]Apomorphine and [³H]Spiperone to Rat Striatal Membranes: Involvement of Surface Phenomena Versus Multiple Binding Sites

Transmembrane Potential and Redox Reactions from a Physiological Point of View

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Surface pharmacology: Drug binding equilibria and ion transport in membrane structures

Cited by 7 publications

References 28 publications

Entropic Trapping Binding Mechanism: Its Likely Role in Receptor−Ligand and Other Biochemical Systems

Entropic Trapping Binding Mechanism: Its Likely Role in Receptor−Ligand and Other Biochemical Systems

Optimal Conditions for [3H]Apomorphine Binding and Anomalous Equilibrium Binding of [3H]Apomorphine and [3H]Spiperone to Rat Striatal Membranes: Involvement of Surface Phenomena Versus Multiple Binding Sites

Transmembrane Potential and Redox Reactions from a Physiological Point of View

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Optimal Conditions for [³H]Apomorphine Binding and Anomalous Equilibrium Binding of [³H]Apomorphine and [³H]Spiperone to Rat Striatal Membranes: Involvement of Surface Phenomena Versus Multiple Binding Sites