Two angiotensin II binding sites in rat brain revealed using [125I]Sar1, Ile8-angiotensin II and selective nonpeptide antagonists.
[125I]Sar1, Ile8 angiotensin II labeled two distinct binding sites in rat brain. The displacement potencies of WL-19, a selective ligand for the angiotensin II subtype 2 receptor, angiotensin II and related peptides indicated that one binding site in the rat brain is the same as the adrenal angiotensin subtype 2 receptor. The second binding site in rat brain was displaced by the selective angiotensin II subtype 1 receptor antagonist DuP-753; however, the displacement potencies of angiotensin II, angiotensin III and Ile7-angiotensin III were significantly less than at the adrenal angiotensin subtype 1 receptor. The data suggests that this binding site in rat brain may represent an angiotensin II receptor subtype which shares some characteristics with the adrenal angiotensin subtype 1 receptor.
Department of New Lead Pharmacology, Merck Sharp and Dohme Research Laboratories, West Point, PA 19486.
R S
RS
Chang
V J
VJ
Lotti
T B
TB
Chen
K A
KA
Faust
D000311:Adrenal Glands / Q000378:metabolism; D000804:Angiotensin II / Q000031:analogs & derivatives* / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D007031:Hypothalamus / Q000378:metabolism; D007700:Kinetics; D008636:Mesencephalon / Q000378:metabolism; D051381:Rats; D011945:Receptors, Angiotensin / Q000378:metabolism*; D013788:Thalamus / Q000378:metabolism
D011945:Receptors, Angiotensin; D000804:Angiotensin II; C009210:sarleucin