Delving into the Latest Updates on SB-206284A with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

VDCCs

Mechanism

VDCCs blockers(Voltage-gated calcium channel blockers)

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication-

Inactive Indication

Stroke

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

SmithKline Beecham Pharmaceuticals Co.

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC25H36ClNO2

InChIKeyGCUITGSHDRSVRS-UHFFFAOYSA-N

CAS Registry154053-02-8

View All Structures (2)

Author: Hamilton, Tom C. ; Hunter, A. Jackie ; Penny D. King ; Price, William J. ; Feuerstein, Giora Z. ; David G. Cooper ; Mark H. Harries ; Karen L. Murkitt ; Tom H. Brown ; Nicole A. Samson ; Campbell, Colin A. ; Benham, Chris D. ; Susan J. Smith ; Roberts, Jenny C. ; Smith, Susan J. ; Barone, Frank C. ; Chris D. Benham ; Sara R. Patel ; Meakin, Jackie E. ; Samson, Nicole A. ; Harries, Mark H. ; Patel, Sara R. ; Murkitt, Karen L. ; Martyn L. Evans ; Alan L. Rothaul ; Evans, Martyn L. ; Wood, Nigel I. ; A. Jackie Hunter ; Tom C. Hamilton ; King, Penny D. ; Cooper, David G. ; Colin A. Campbell ; Jackie E. Meakin ; Rothaul, Alan L. ; Brown, Tom H. ; Jenny C. Roberts

The effects of SB 206284A, 1-[7-(4-benzyloxyphenoxy)heptyl] piperidine hydrochloride, have been investigated in vitro on calcium and sodium currents in rat-cultured dorsal root ganglion (DRG) neurones and potassium-mediated calcium influx in rat synaptosomes. Cardiovascular hemodynamic effects in both anesthetized and conscious rats, and neuroprotective activity in in vivo cerebral ischemia models were also investigated. In the rat DRG cells, SB 206284A caused almost complete block of the sustained inward Ca2+ current (IC50 = 2.4μM), suggesting that the compound is an effective blocker of slowly inactivating, high-voltage calcium current. SB 206284A reduced locomotor hyperactivity in the gerbil bilateral carotid artery occlusion model without affecting ischemia-induced damage in the hippocampal CA1 region. In the rat middle cerebral artery occlusion model, SB 206284A reduced lesion volume in the posterior forebrain, and in the rat photochemical cortical lesion model, lesion volume was reduced even when treatment was delayed until 4 hours after occlusion. At neuroprotective doses, SB 206284A had no cardiovascular effects. These findings show that SB 206284A is a novel calcium channel antagonist that shows neuroprotective properties.

100 Deals associated with SB-206284A

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