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

Abstract

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.

Inventors:
;
Issue Date:
Research Org.:
Univ. of California, Oakland, CA (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1176335
Patent Number(s):
7731940
Application Number:
11/626,797
Assignee:
The Regents of the University of California (Oakland, CA)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07D - HETEROCYCLIC COMPOUNDS
DOE Contract Number:  
FG03-02ER63294
Resource Type:
Patent
Resource Relation:
Patent File Date: 2007 Jan 24
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; 60 APPLIED LIFE SCIENCES

Citation Formats

Mukherjee, Jogeshwar, and Saigal, Neil. Compositions and methods related to serotonin 5-HT1A receptors. United States: N. p., 2010. Web.
Mukherjee, Jogeshwar, & Saigal, Neil. Compositions and methods related to serotonin 5-HT1A receptors. United States.
Mukherjee, Jogeshwar, and Saigal, Neil. Tue . "Compositions and methods related to serotonin 5-HT1A receptors". United States. https://www.osti.gov/servlets/purl/1176335.
@article{osti_1176335,
title = {Compositions and methods related to serotonin 5-HT1A receptors},
author = {Mukherjee, Jogeshwar and Saigal, Neil},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2010},
month = {6}
}

Works referenced in this record:

Therapeutic strategies for the treatment of stroke
journal, August 2006


Potential therapeutic targets for schizophrenia
journal, December 1999


Serotonin 1A receptors in the living brain of Alzheimer's disease patients
journal, January 2006


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