Neuronal N-type calcium channel blockers: a series of 4-piperidinylaniline analogs with analgesic activity

L Y Hu; T R Ryder; M F Rafferty; K M Siebers; T Malone; A Chatterjee; M R Feng; S M Lotarski; D M Rock; S J Stoehr; C P Taylor; M L Weber; G P Miljanich; E Millerman; B G Szoke

Neuronal N-type calcium channel blockers: a series of 4-piperidinylaniline analogs with analgesic activity

Drug Des Discov. 2000;17(1):85-93.

Authors

L Y Hu¹, T R Ryder, M F Rafferty, K M Siebers, T Malone, A Chatterjee, M R Feng, S M Lotarski, D M Rock, S J Stoehr, C P Taylor, M L Weber, G P Miljanich, E Millerman, B G Szoke

Affiliation

¹ Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.

PMID: 10928451

Abstract

Several novel N-type voltage sensitive calcium channel blockers showed high affinity in the IMR32 assay and efficacy in the anti-writhing model. Herein, we describe the design, synthesis, SAR studies, biological data, physicochemical properties and pharmacokinetics of this 4-piperidinylaniline series.

MeSH terms

Analgesics, Non-Narcotic / pharmacology*
Aniline Compounds / pharmacology*
Animals
Calcium Channel Blockers / chemical synthesis
Calcium Channel Blockers / pharmacology*
Calcium Channels, N-Type / drug effects*
Mice
Structure-Activity Relationship

Substances

Analgesics, Non-Narcotic
Aniline Compounds
Calcium Channel Blockers
Calcium Channels, N-Type