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Title: Compositions and methods related to serotonin 5-HT1A receptors

Patent ·
OSTI ID:1176335

Contemplated substituted arylpiperazinyl compounds, and most preferably 18F-Mefway, exhibit desirable in vitro and in vivo binding characteristics to the 5-HT1A receptor. Among other advantageous parameters, contemplated compounds retain high binding affinity, display optimal lipophilicity, and are radiolabeled efficiently with 18F-fluorine in a single step. Still further, contemplated compounds exhibit high target to non-target ratios in receptor-rich regions both in vitro and in vivo, and selected compounds can be effectively and sensitively displaced by serotonin, thus providing a quantitative tool for measuring 5-HT1A receptors and serotonin concentration changes in the living brain.

Research Organization:
Univ. of California, Oakland, CA (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
FG03-02ER63294
Assignee:
The Regents of the University of California (Oakland, CA)
Patent Number(s):
7,731,940
Application Number:
11/626,797
OSTI ID:
1176335
Resource Relation:
Patent File Date: 2007 Jan 24
Country of Publication:
United States
Language:
English

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The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders journal August 2005
Compounds Labelled with Short-Lived beta+-Emitting Radionuclides and Some Applications in Life Sciences. The Importance of Time as a Parameter. journal January 1999
Development of Fluorine-18-Labeled 5-HT 1A Antagonists journal May 1999
In vivo Measurement of the Serotonin Transporter with (S)-([18F]fluoromethyl)-(+)-McN5652 journal June 2003