2. Academic Validation
  3. N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

  • Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12. doi: 10.1016/s0960-894x(99)00100-6.
L Y Hu 1,  T R Ryder,  M F Rafferty,  W L Cody,  S M Lotarski,  G P Miljanich,  E Millerman,  D M Rock,  Y Song,  S J Stoehr,  C P Taylor,  M L Weber,  B G Szoke,  M G Vartanian
Affiliations

Affiliation

  • 1 Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
PMID: 10206559 DOI: 10.1016/s0960-894x(99)00100-6
Abstract

Selective N-type voltage sensitive Calcium Channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.

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