S-Emopamil, a novel calcium channel blocker and serotonin S2 antagonist, markedly reduces infarct size following middle cerebral artery occlusion in the rat

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Abstract

(S)-Emopamil is a novel calcium channel blocker of the phenylalkylalanine class, with superior blood-brain permeability and potent serotonin S2 antagonist activity. In this study, we investigated the effects of (S)-emopamil on the histopathologic consequences of permanent middle cerebral artery (MCA) occlusion in anesthetized Sprague-Dawley rats. In three treatment protocols, intraperitoneal (S)-emopamil therapy was begun either 30 minutes prior to, immediately after, or 1 hour after MCA occlusion. Nontreated and saline-treated control groups were also studied. Cortical infarct volumes in nontreated and saline-treated control rats were 85 ± 22 and 66 ± 19 mm3 (mean ± SD), respectively, and did not differ statistically from one another. Corresponding cortical infarct volume values in (S)-emopamil-pretreated rats, and in rats with post-treatment at 0 hours and 1 hour, were 33 ± 23, 29 ± 14, and 27 ± 16 mm3, respectively; each of these was significantly smaller than control values. In contrast to the neocortex, striatal infarct volume was not altered by (S)-emopamil treatment. The results of this study demonstrate the marked therapeutic efficacy of (S)-emopamil in focal cortical infarction, even when treatment is delayed for 1 hour following MCA occlusion.

Original languageEnglish
Pages (from-to)1667-1673
Number of pages7
JournalNeurology
Volume38
Issue number11
StatePublished - Jan 1 1988

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Serotonin Antagonists
Middle Cerebral Artery Infarction
Calcium Channel Blockers
Therapeutics
Corpus Striatum
Neocortex
Clinical Protocols
Infarction
Sprague Dawley Rats
emopamil
Permeability
Control Groups
Brain

ASJC Scopus subject areas

  • Neuroscience(all)

Cite this

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title = "S-Emopamil, a novel calcium channel blocker and serotonin S2 antagonist, markedly reduces infarct size following middle cerebral artery occlusion in the rat",
abstract = "(S)-Emopamil is a novel calcium channel blocker of the phenylalkylalanine class, with superior blood-brain permeability and potent serotonin S2 antagonist activity. In this study, we investigated the effects of (S)-emopamil on the histopathologic consequences of permanent middle cerebral artery (MCA) occlusion in anesthetized Sprague-Dawley rats. In three treatment protocols, intraperitoneal (S)-emopamil therapy was begun either 30 minutes prior to, immediately after, or 1 hour after MCA occlusion. Nontreated and saline-treated control groups were also studied. Cortical infarct volumes in nontreated and saline-treated control rats were 85 ± 22 and 66 ± 19 mm3 (mean ± SD), respectively, and did not differ statistically from one another. Corresponding cortical infarct volume values in (S)-emopamil-pretreated rats, and in rats with post-treatment at 0 hours and 1 hour, were 33 ± 23, 29 ± 14, and 27 ± 16 mm3, respectively; each of these was significantly smaller than control values. In contrast to the neocortex, striatal infarct volume was not altered by (S)-emopamil treatment. The results of this study demonstrate the marked therapeutic efficacy of (S)-emopamil in focal cortical infarction, even when treatment is delayed for 1 hour following MCA occlusion.",
author = "H. Nakayama and Myron Ginsberg and {Dalton Dietrich}, W.",
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T1 - S-Emopamil, a novel calcium channel blocker and serotonin S2 antagonist, markedly reduces infarct size following middle cerebral artery occlusion in the rat

AU - Nakayama, H.

AU - Ginsberg, Myron

AU - Dalton Dietrich, W.

PY - 1988/1/1

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N2 - (S)-Emopamil is a novel calcium channel blocker of the phenylalkylalanine class, with superior blood-brain permeability and potent serotonin S2 antagonist activity. In this study, we investigated the effects of (S)-emopamil on the histopathologic consequences of permanent middle cerebral artery (MCA) occlusion in anesthetized Sprague-Dawley rats. In three treatment protocols, intraperitoneal (S)-emopamil therapy was begun either 30 minutes prior to, immediately after, or 1 hour after MCA occlusion. Nontreated and saline-treated control groups were also studied. Cortical infarct volumes in nontreated and saline-treated control rats were 85 ± 22 and 66 ± 19 mm3 (mean ± SD), respectively, and did not differ statistically from one another. Corresponding cortical infarct volume values in (S)-emopamil-pretreated rats, and in rats with post-treatment at 0 hours and 1 hour, were 33 ± 23, 29 ± 14, and 27 ± 16 mm3, respectively; each of these was significantly smaller than control values. In contrast to the neocortex, striatal infarct volume was not altered by (S)-emopamil treatment. The results of this study demonstrate the marked therapeutic efficacy of (S)-emopamil in focal cortical infarction, even when treatment is delayed for 1 hour following MCA occlusion.

AB - (S)-Emopamil is a novel calcium channel blocker of the phenylalkylalanine class, with superior blood-brain permeability and potent serotonin S2 antagonist activity. In this study, we investigated the effects of (S)-emopamil on the histopathologic consequences of permanent middle cerebral artery (MCA) occlusion in anesthetized Sprague-Dawley rats. In three treatment protocols, intraperitoneal (S)-emopamil therapy was begun either 30 minutes prior to, immediately after, or 1 hour after MCA occlusion. Nontreated and saline-treated control groups were also studied. Cortical infarct volumes in nontreated and saline-treated control rats were 85 ± 22 and 66 ± 19 mm3 (mean ± SD), respectively, and did not differ statistically from one another. Corresponding cortical infarct volume values in (S)-emopamil-pretreated rats, and in rats with post-treatment at 0 hours and 1 hour, were 33 ± 23, 29 ± 14, and 27 ± 16 mm3, respectively; each of these was significantly smaller than control values. In contrast to the neocortex, striatal infarct volume was not altered by (S)-emopamil treatment. The results of this study demonstrate the marked therapeutic efficacy of (S)-emopamil in focal cortical infarction, even when treatment is delayed for 1 hour following MCA occlusion.

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