Peptidic endothelin-1 receptor antagonist, BQ-123, and neuroprotection.
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.
Feuerstein
G
G
Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406.
Gu
J L
JL
Ohlstein
E H
EH
Barone
F C
FC
Yue
T L
TL
D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000502:physiology*; D005849:Gerbillinae; D006624:Hippocampus / Q000098:blood supply / Q000187:drug effects*; D002546:Ischemic Attack, Transient / Q000517:prevention & control*; D008297:Male; D009474:Neurons / Q000187:drug effects*; D010456:Peptides, Cyclic / Q000494:pharmacology*
D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D010456:Peptides, Cyclic; C072247:cyclo(Trp-Asp-Pro-Val-Leu)