Abstract：
:In the present studies, we have examined the effects of two new Ca(2+) channel blockers, LY042826 (N-[2-[(2-methylphenyl)(phenyl)methoxy]ethyl]-1-butanamine hydrochloride) and LY393615 (N-[[5, 5-bis(4-fluorophenyl)tetrahydro-2-furanyl]methyl]-1-butanamine hydrochloride) in the gerbil model of global and the endothelin-1 rat model of focal cerebral ischaemia in vivo. Results indicated that both LY042826 (P<0.01) and LY393615 (P<0.001) provided significant protection against ischaemia-induced hippocampal damage in global cerebral ischaemia when dosed at 15 mg/kg i.p. 30 min before and 2 h 30 min after occlusion. In further studies, LY042826 (P<0.05) and LY393615 (P<0.01) were also protective when administered at 15 mg/kg i.p. immediately after and 3 h post-occlusion. Both compounds also provided a significant reduction in the infarct volume following endothelin-1 middle cerebral artery occlusion in the rat when administered at 15 mg/kg i.p. immediately (P<0.05) after occlusion. This protection was similar to that observed with the NMDA receptor antagonist (5R,10S)-(+)-5-methyl-10, 11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine), MK-801 in this model. In conclusion and as a result of the present studies, we report that the novel Ca(2+) channel blockers, LY042826 and LY393615 protect against ischaemia-induced brain injury in gerbils and rats. The compounds were neuroprotective when administered post-occlusion and may therefore be useful anti-ischaemic agents.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Hicks CA,Ward MA,O'Neill MJdoi
10.1016/s0014-2999(00)00784-6keywords:
subject
Has Abstractpub_date
2000-11-24 00:00:00pages
241-8issue
3eissn
0014-2999issn
1879-0712pii
S0014299900007846journal_volume
408pub_type
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