2. Academic Validation
  3. Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry

Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry

  • Bioorg Med Chem Lett. 2004 Aug 2;14(15):4031-5. doi: 10.1016/j.bmcl.2004.05.031.
Dimitrios Galanakis 1,  C Robin Ganellin
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 541 24 Thessaloniki, Greece. dgalana@pharm.auth.gr
PMID: 15225721 DOI: 10.1016/j.bmcl.2004.05.031
Abstract

QSAR studies of a series of blockers of the SK(CA) channel in guinea-pig hepatocytes suggests that the polarizability of the blocker is an important factor controlling the binding to the channel. It is suggested that, upon binding, an ion-pair is formed, a process that is promoted by the reorganization of the water molecules. The polarizability is not adequate to describe the potency of the most potent blockers with a good stereochemical fit to the channel, presumably due to more specific interactions taking place.

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