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.
D000284:Administration, Oral; D047228:Angiotensin II Type 1 Receptor Blockers; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001562:Benzimidazoles / Q000494:pharmacology / Q000627:therapeutic use*; D001713:Biphenyl Compounds; D001812:Blood-Brain Barrier / Q000187:drug effects; D002545:Brain Ischemia / Q000188:drug therapy*; D009473:Neuronal Plasticity / Q000187:drug effects; D051381:Rats; D013777:Tetrazoles / Q000494:pharmacology / Q000627:therapeutic use*
D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001713:Biphenyl Compounds; D013777:Tetrazoles; C081643:candesartan