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Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.
Authors:R M Schelkun  P Yuen  T C Malone  D M Rock  S Stoehr  B Szoke  K Tarczy-Hornoch
Institution:Parke-Davis Pharmaceutical Research Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Abstract:Voltage activated calcium channel (VACC) blockers have been demonstrated to have utility in the treatment of stroke and pain. A series of aminomethyl substituted phenol derivatives has been identified with good functional activity and selectivity for N-type VACC's over sodium and potassium channels. The methods of synthesis and preliminary pharmacology are discussed herein.
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