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Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.

Abstract：

:Radioligands are powerful tools for examining the pharmacological profiles of chemical leads and thus facilitate drug discovery. In this study, we identified and characterized 3-([1,1,1-(3)H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy} phenyl)-4(3H)-quinazolinone ([(3)H]1) as a potent and selective radioligand for histamine H(3) receptors. Radioligand [(3)H]1 exhibited appreciable specific signal in brain slices prepared from wild-type mice but not from histamine H(3) receptor-deficient mice, demonstrating the specificity and utility of [(3)H]1 as a selective histamine H(3) receptor radioligand for ex-vivo receptor occupancy assays.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Mitobe Y,Ito S,Mizutani T,Nagase T,Sato N,Tokita S

doi

10.1016/j.bmcl.2009.06.025

subject

Has Abstract

pub_date

2009-08-01 00:00:00

pages

4075-8

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00856-7

journal_volume

19

pub_type

杂志文章

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