Intrinsic association constants were determined for a series of aminopyridines on phosphatidylserine vesicles, through determination of electrophoretic mobility. The magnitudes of the constants were such that depolarization of the nerve terminal through binding to negative phospholipids seems unlikely to occur. The aminopyridines all had association constants between one half and one sixtieth the association constant of calcium. The aminopyridines probably block potassium channels in their enhancement of synaptic transmission.
An interesting correlation was noted in that the ranking of the aminopyridines in terms of their affinity for these lipids was approximately the same as the ranking of their enhancement of synaptic transmission in a wide variety of biological preparations. A possible mechanism for this correlation is that adsorption of these drugs 2 to lipid membranes is the initial and rate-limiting step in their action.
| Identifer | oai:union.ndltd.org:pdx.edu/oai:pdxscholar.library.pdx.edu:open_access_etds-4695 |
| Date | 01 January 1986 |
| Creators | Wright, Colin |
| Publisher | PDXScholar |
| Source Sets | Portland State University |
| Detected Language | English |
| Type | text |
| Format | application/pdf |
| Source | Dissertations and Theses |
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