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

Abstract

Contemplated substituted arylpiperazinyl compounds, and most preferably .sup.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 .sup.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.

Inventors:
 [1];  [2];  [3]
  1. Irvine, CA
  2. Fresno, CA
  3. (Fresno, CA)
Issue Date:
Research Org.:
Lawrence Livermore National Lab. (LLNL), Livermore, CA (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1062976
Patent Number(s):
RE43,688
Assignee:
The Regents of the University of California (Oakland, CA)
DOE Contract Number:  
FG03-02ER63294
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
60 APPLIED LIFE SCIENCES

Citation Formats

Mukherjee, Jogeshwar, Saigal, Neil, and Saigal, legal representative, Harsh. Compositions and methods related to serotonin 5-HT1A receptors. United States: N. p., 2012. Web.
Mukherjee, Jogeshwar, Saigal, Neil, & Saigal, legal representative, Harsh. Compositions and methods related to serotonin 5-HT1A receptors. United States.
Mukherjee, Jogeshwar, Saigal, Neil, and Saigal, legal representative, Harsh. Tue . "Compositions and methods related to serotonin 5-HT1A receptors". United States. https://www.osti.gov/servlets/purl/1062976.
@article{osti_1062976,
title = {Compositions and methods related to serotonin 5-HT1A receptors},
author = {Mukherjee, Jogeshwar and Saigal, Neil and Saigal, legal representative, Harsh},
abstractNote = {Contemplated substituted arylpiperazinyl compounds, and most preferably .sup.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 .sup.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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2012},
month = {9}
}

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