Peptidic endothelin-1 receptor antagonist, BQ-123, and neuroprotection

G Feuerstein; J L Gu; E H Ohlstein; F C Barone; T L Yue

doi:10.1016/0196-9781(94)90207-0

Peptidic endothelin-1 receptor antagonist, BQ-123, and neuroprotection

Peptides. 1994;15(3):467-9. doi: 10.1016/0196-9781(94)90207-0.

Authors

G Feuerstein¹, J L Gu, E H Ohlstein, F C Barone, T L Yue

Affiliation

¹ Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406.

PMID: 7937321
DOI: 10.1016/0196-9781(94)90207-0

Abstract

Endothelin-1 (ET-1) is a potent cerebrovascular constrictor that has been implicated in brain ischemia. Utilizing the ETA receptor antagonist, BQ-123, the role of ET-1 in ischemic neuronal death following global ischemia was studied. BQ-123, administered ICV, either before and after ischemia or only after ischemia, increased hippocampal CA1 neuron survival in gerbils subjected to transient global ischemia. This study suggests that ETA receptor antagonists might be useful in neuronal salvage following stroke.

MeSH terms

Animals
Body Temperature / drug effects
Endothelin Receptor Antagonists*
Endothelins / physiology*
Gerbillinae
Hippocampus / blood supply
Hippocampus / drug effects*
Ischemic Attack, Transient / prevention & control*
Male
Neurons / drug effects*
Peptides, Cyclic / pharmacology*

Substances

Endothelin Receptor Antagonists
Endothelins
Peptides, Cyclic
cyclo(Trp-Asp-Pro-Val-Leu)