288573-58-0Relevant academic research and scientific papers
The discovery of [1-(4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phenyl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Taylor, Charles P.,Feng, M. Rose,Kuo, Be-Sheng,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Siebers, Krista M.,Szoke, Balazs G.
, p. 1203 - 1212 (2007/10/03)
Our drug discovery efforts for N-type calcium channel blockers in the 4-piperidinylaniline series led to the discovery of an orally active analgesic agent 26. 1-[4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethyl-butyl)-phenyl]-(3-methyl-but-2-enyl)-amine (26) showed high affinity to functionally block N-type calcium channels (IC50=0.7 μM in the IMR32 assay) and exhibited high efficacy in the anti-writhing analgesia test with mice (ED50=12 mg/kg by po and 4 mg/kg by iv). In this report, the rationale for the design, synthesis, biological evaluation, and pharmacokinetics of this series of blockers is described. Copyright (C) 2000 Elsevier Science Ltd.
Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists
Ryder, Todd R.,Hu, Lain-Yen,Rafferty, Michael F.,Lotarski, Susan M.,Rock, David M.,Stoehr, Sally J.,Taylor, Charles P.,Weber, Mark L.,Miljanich, George P.,Millerman, Elizabeth,Szoke, Balazs G.
, p. 2453 - 2458 (2007/10/03)
Selective N-Type Voltage Sensitive Calcium Channel (VSCC) antagonists have shown utility in several models of pain and ischemia. We report the structure-activity relationship at the proximal phenyl group in a series of non-peptidyl VSCC blockers.
