Heterogeneity of angiotensin II AT2 receptors in the rat brain.
Angiotensin II (AT) receptor subtypes (AT1, selectively displaced by DuP 753, and AT2, selectively displaced by PD123177 and CGP42112A) were characterized by quantitative autoradiography after incubation with the AT agonist 125I-Sar1-AT, in specific brain nuclei of young (2-week-old) rats. Binding to AT1 receptors was sensitive (decreased affinity) to incubation in the presence of guanosine 5'-O-(3-thio)triphosphate (GTP gamma S). Only the AT1 receptors in the paraventricular nucleus were sensitive to pertussis toxin, indicating the possibility of the existence of AT1 receptor subtypes. The sensitivity of AT2 receptors to GTP gamma S was heterogeneous. In the ventral thalamic and medial geniculate nuclei and in the locus coeruleus, binding to AT2 receptors was sensitive to GTP gamma S and to pertussis toxin pretreatment. Conversely, in the inferior olive, binding was insensitive to GTP gamma S and to pertussis toxin pretreatment. We propose the nomenclature of AT2A receptors for those receptors sensitive to guanine nucleotides and pertussis toxin and that of AT2B receptors for those showing no sensitivity to guanine nucleotides or pertussis toxin treatment.
Tsutsumi
K
K
Section on Pharmacology, National Institute of Mental Health, Bethesda, Maryland 20892.
Saavedra
J M
JM
D000804:Angiotensin II / Q000378:metabolism*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000648:ultrastructure*; D005260:Female; D006150:Guanine Nucleotides / Q000494:pharmacology; D008297:Male; D037342:Pertussis Toxin; D051381:Rats; D011919:Rats, Inbred Strains; D011945:Receptors, Angiotensin / Q000145:classification* / Q000378:metabolism; D013997:Time Factors; D010566:Virulence Factors, Bordetella / Q000494:pharmacology
D057911:Angiotensin Receptor Antagonists; D006150:Guanine Nucleotides; D011945:Receptors, Angiotensin; D010566:Virulence Factors, Bordetella; D000804:Angiotensin II; D037342:Pertussis Toxin