Inhibiting angiotensin receptors in the brain: possible therapeutic implications

Although the angiotensin AT1-receptor is known to be involved in cognitive function, its potential role in neuroplasticity is unclear. Animal studies to date have shown that only an effective blockade of brain AT1-receptors has neuroprotective effects in ischaemic neuronal tissue and improves the neurological outcome of focal brain ischaemia. The requirements for such an antagonist include sufficient penetration to cross the blood-brain barrier when administered orally, effective and selective inhibition of AT1-receptors in the brain, and long-lasting receptor blockade. Candesartan was the most effective angiotensin receptor blocker (ARB) in crossing the blood-brain barrier.