Targeting endothelin receptors for pharmacotherapy of ischemic stroke: current scenario and future perspectives

Increased expression of endothelin (ET) peptide and its receptors following ischemic stroke is found to regulate many critical aspects of stroke pathophysiology. Many attempts have been made to target ET receptors in various animal models of stroke, but it is very difficult to draw a definite line o...

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Bibliographic Details
Published in:Drug discovery today 2012-07, Vol.17 (13-14), p.793-804
Main Authors: Kaundal, Ravinder K., Deshpande, Tushar A., Gulati, Anil, Sharma, Shyam S.
Format: Article
Language:English
Subjects:
Animal models
Animals
Biological and medical sciences
Brain Ischemia - complications
Brain Ischemia - drug therapy
Disease Models, Animal
Drug Discovery - methods
Drug Discovery - trends
Endothelin Receptor Antagonists
General pharmacology
Humans
Medical sciences
Neuroprotective Agents - administration & dosage
Neuroprotective Agents - adverse effects
Neuroprotective Agents - therapeutic use
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Receptors, Endothelin - agonists
Receptors, Endothelin - genetics
Receptors, Endothelin - metabolism
Signal Transduction
Stroke - drug therapy
Stroke - etiology
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Summary:Increased expression of endothelin (ET) peptide and its receptors following ischemic stroke is found to regulate many critical aspects of stroke pathophysiology. Many attempts have been made to target ET receptors in various animal models of stroke, but it is very difficult to draw a definite line of conclusion, because these studies differ in many aspects, such as animal model, treatment schedule, parameters and techniques used for assessing these parameters. A meta-analysis of all studies showed a significant reduction in the lesion volume and improvement in functional outcome in focal cerebral ischemia. ETA receptor antagonists appear to offer an essential advantage of multiple neuroprotective mechanisms, including prevention of blood–brain barrier disruption and leukocyte infiltration.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2012.02.017