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Radioiodinated CGP 42112A: A Novel High Affinity and Highly Selective Ligand for the Characterization of Angiotensin AT2 Receptors

Radioiodinated CGP 42112A: A Novel High Affinity and Highly Selective Ligand for the Characterization of Angiotensin AT2 Receptors

S E Whitebread, V Taylor, S P Bottari, B Kamber, M de Gasparo

Biochem Biophys Res Commun. 1991 Dec 31;181(3):1365-71.

PMID: 1764088

Abstract:

CGP 42112A, a potent angiotensin AT2 receptor selective ligand, was radio-iodinated and its binding characteristics compared with those of [125I]angiotensin II. In human myometrium (only AT2 expressed), binding was saturable (Kd 1.03 x 10(-10) M; Bmax 807 fmol/mg) and reversible (K+1 1.89 x 10(8) M-1.min-1; K-1 3.77 x 10(-3) min-1). The order of potency of a number of peptides and non-peptides was the same as when [125I] angiotensin II was used as tracer. No specific binding could be detected on membranes from vascular smooth muscle cells (only AT1 expressed). In rat adrenal glomerulosa membranes (mixed AT1/AT2), [125I]CGP 42112A bound only to AT2. [125I]CGP 42112A can therefore be used as a specific probe for AT2 receptors and will be especially useful in tissues where other subtypes are also present.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP127060757	CGP-42112A		127060-75-7	Price

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