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3 results on '"T R, Ryder"'

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

Author

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, and B G, Szoke

Subjects
Mice, Structure-Activity Relationship, Aniline Compounds, Calcium Channels, N-Type, Animals, Analgesics, Non-Narcotic, Calcium Channel Blockers
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.

Published
2000

3. Structure-activity relationship at the leucine side chain in a series of N,N-dialkyldipeptidyl-amines as N-type calcium channel blockers

Author

T R, Ryder, L Y, Hu, M F, Rafferty, S M, Lotarski, D M, Rock, S J, Stoehr, C P, Taylor, M L, Weber, G P, Miljanich, E, Millerman, and B G, Szoke

Subjects
Electrophysiology, Structure-Activity Relationship, Calcium Channels, N-Type, Solubility, Leucine, Alkanes, Dipeptides, Calcium Channel Blockers, Oligopeptides, omega-Conotoxins
Abstract

Exploration of the SAR around the leucine side chain in a series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC is presented. A novel analog is disclosed which possesses improved aqueous solubility, in vivo activity in an audiogenic seizure model, and reversible blockade in electrophysiological assays.

Published
2000

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