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Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.

Abstract：

:The chemical synthesis of 2-[(2,6-dichloro-4-iodophenyl)imino]imidazolidine (PIC) and its radioiodinated analogue [125I]PIC is described. PIC was synthesized from 2,6-dichloroaniline in five synthetic steps. This agent displayed a high affinity for the alpha 2-adrenergic receptor (IC50 = 1.5 nM) in competitive binding assays conducted with purified human platelet plasma membrane fractions. For the synthesis of radioiodinated PIC the triazene intermediate 11 was synthesized from 2,6-dichloro-4-nitroaniline in five synthetic steps. Acid-catalyzed decomposition of 11 with no-carrier-added Na125I afforded high specific activity [125I]PIC. In view of its high affinity for the alpha 2-adrenergic receptor, [125I]PIC is a potentially useful probe for studies in adrenergic pharmacology.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Van Dort M,Neubig R,Counsell RE

doi

10.1021/jm00390a021

subject

Has Abstract

pub_date

1987-07-01 00:00:00

pages

1241-4

issue

7

eissn

0022-2623

issn

1520-4804

journal_volume

30

pub_type

杂志文章

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