Functional evidence for the ability of angiotensin AT1 receptor antagonists to cross the blood-brain barrier in rats

European Journal of Pharmacology
C PolidoriM Massi


The angiotensin AT1 receptor antagonists, losartan (2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'(1H-tetrazol-5-yl)biphen yl-4- yl)methyl]imidazole potassium salt), EXP3174 (2-n-butyl-4-chloro-1-[(2'(1 H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole-5-carboxylic acid), GR117289 (1-[[3-bromo-2-[2-(1 H-tetrazol-5-yl)phenyl]-5-benzofuranyl]methyl]-2-butyl-4-chloro-1 H-imidazole-5-carboxylic acid) and LR-B/081 (methyl-2-[[4-butyl-2-methyl-6-oxo-5-[[2'-(1 H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1(6H)-pyrimidinyl]met hyl]-3- thiophenecarboxylate), given by intraperitoneal (i.p.) injection 15 min before intracerebroventricular administration of angiotensin II, inhibited drinking with the following order of potency: EXP3174 > GR117289 > losartan > LR-B/081. When 20 mumol/kg of each antagonist was i.p. injected 15 min, 4, 12 or 24 h before angiotensin II, EXP3174 and GR117289 inhibited water intake at each observation time, losartan at 4, 12 and 24 h, LR-B/081 only at 4 and 12 h. After per os administration of the same dose 4 or 12 h before angiotensin II, losartan reduced drinking at 4, but not at 12 h; LR-B/081 did not inhibit drinking either at 4 or 12 h. The present results suggest that EXP3174 and GR117289 cross the barrier readily...Continue Reading


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