Characterization of brain angiotensin II AT2 receptor subtype using [125I] CGP 42112A. 1993

F M Heemskerk, and S Zorad, and A Seltzer, and J M Saavedra
Section on Pharmacology, NIMH, Bethesda, MD 20892.

Recently two subtypes of angiotensin receptors have been described, AT1 and AT2. Currently used radiolabeled agonists and antagonists are not able to discriminate between these receptors subtypes. Here we characterize the use of [125I] CGP 42112A, a novel, specific ligand for AT2 receptors, in a membrane binding assay and in autoradiography of brain sections of 2 week old rats. [125I] CGP 42112A bound with high affinity and autoradiography revealed binding selectively localized to areas known to express the AT2 receptor subtype only. CGP 42112A, angiotensin II, angiotensin III and PD 123177 competed for [125I] CGP 42112A binding, with potencies consistent with high affinity and specific binding to AT2 receptors. Thus [125I] CGP 42112A will be a useful new tool to study AT2 receptors.

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D011725 Pyridines Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
D011945 Receptors, Angiotensin Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells. Angiotensin Receptor,Angiotensin Receptors,Angiotensin II Receptor,Angiotensin III Receptor,Receptor, Angiotensin II,Receptor, Angiotensin III,Receptor, Angiotensin
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D005260 Female Females
D005829 Geniculate Bodies Part of the DIENCEPHALON inferior to the caudal end of the dorsal THALAMUS. Includes the lateral geniculate body which relays visual impulses from the OPTIC TRACT to the calcarine cortex, and the medial geniculate body which relays auditory impulses from the lateral lemniscus to the AUDITORY CORTEX. Lateral Geniculate Body,Medial Geniculate Body,Metathalamus,Corpus Geniculatum Mediale,Geniculate Nucleus,Lateral Geniculate Nucleus,Medial Geniculate Complex,Medial Geniculate Nucleus,Nucleus Geniculatus Lateralis Dorsalis,Nucleus Geniculatus Lateralis Pars Dorsalis,Bodies, Geniculate,Complex, Medial Geniculate,Complices, Medial Geniculate,Corpus Geniculatum Mediales,Geniculate Bodies, Lateral,Geniculate Bodies, Medial,Geniculate Body,Geniculate Body, Lateral,Geniculate Body, Medial,Geniculate Complex, Medial,Geniculate Complices, Medial,Geniculate Nucleus, Lateral,Geniculate Nucleus, Medial,Geniculatum Mediale, Corpus,Geniculatum Mediales, Corpus,Lateral Geniculate Bodies,Medial Geniculate Bodies,Medial Geniculate Complices,Mediale, Corpus Geniculatum,Mediales, Corpus Geniculatum,Nucleus, Geniculate,Nucleus, Lateral Geniculate,Nucleus, Medial Geniculate
D000804 Angiotensin II An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS. Angiotensin II, Ile(5)-,Angiotensin II, Val(5)-,5-L-Isoleucine Angiotensin II,ANG-(1-8)Octapeptide,Angiotensin II, Isoleucine(5)-,Angiotensin II, Valine(5)-,Angiotensin-(1-8) Octapeptide,Isoleucine(5)-Angiotensin,Isoleucyl(5)-Angiotensin II,Valyl(5)-Angiotensin II,5 L Isoleucine Angiotensin II,Angiotensin II, 5-L-Isoleucine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001345 Autoradiography The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed) Radioautography

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