Angiotensin II receptor subtypes in rat brain: dithiothreitol inhibits ligand binding to AII-1 and enhances binding to AII-2.
Angiotensin II (AII) receptor subtypes have been proposed on the basis of the selectivity of non-peptide AII antagonists. In the present study, the sulfhydryl reducing agent dithiothreitol (DTT) was found to reduce binding to the AII-1 receptor while enhancing binding at the AII-2 site. The neuroanatomical distribution of these effects were consistent with the distribution of AII-1 and AII-2 receptors, respectively. These data indicate that AII receptor subtypes in the brain can be differentiated by both biochemical and pharmacological means.
Gehlert
D R
DR
Central Nervous System Research, Eli Lilly and Company, Indianapolis, IN 46285.
Gackenheimer
S L
SL
Schober
D A
DA
D000804:Angiotensin II / Q000037:antagonists & inhibitors / Q000378:metabolism*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D001345:Autoradiography; D001923:Brain Chemistry / Q000187:drug effects*; D004229:Dithiothreitol / Q000494:pharmacology*; D007093:Imidazoles / Q000494:pharmacology; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D019808:Losartan; D008297:Male; D011725:Pyridines / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011945:Receptors, Angiotensin / Q000378:metabolism*; D012504:Saralasin / Q000378:metabolism; D013777:Tetrazoles / Q000494:pharmacology
D057911:Angiotensin Receptor Antagonists; D007093:Imidazoles; D007457:Iodine Radioisotopes; D011725:Pyridines; D011945:Receptors, Angiotensin; D013777:Tetrazoles; D000804:Angiotensin II; C063457:WL 19; D012504:Saralasin; D019808:Losartan; D004229:Dithiothreitol