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}
}
Save to My Library
You must Sign In or Create an Account in order to save documents to your library.
Works referenced in this record:
Therapeutic strategies for the treatment of stroke
journal, August 2006
- Green, A. Richard; Shuaib, Ashfaq
- Drug Discovery Today, Vol. 11, Issue 15-16
A retrospect on the discovery of way-100635 and the prospect for improved 5-HT1A receptor PET radioligands
journal, July 2000
- Cliffe, Ian A.
- Nuclear Medicine and Biology, Vol. 27, Issue 5
Potential therapeutic targets for schizophrenia
journal, December 1999
- Wong, Albert HC; Sanyal, Suparna; Knapp, Mark GL
- Emerging Therapeutic Targets, Vol. 3, Issue 4
Serotonin 1A receptors in the living brain of Alzheimer's disease patients
journal, January 2006
- Kepe, V.; Barrio, J. R.; Huang, S. -C.
- Proceedings of the National Academy of Sciences, Vol. 103, Issue 3
The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders
journal, August 2005
- Grigoriadis, Dimitri E.
- Expert Opinion on Therapeutic Targets, Vol. 9, Issue 4
Compounds Labelled with Short-Lived beta+-Emitting Radionuclides and Some Applications in Life Sciences. The Importance of Time as a Parameter.
journal, January 1999
- Långström, Bengt; Kihlberg, Tor; Bergström, Mats
- Acta Chemica Scandinavica, Vol. 53
Development of Fluorine-18-Labeled 5-HT 1A Antagonists
journal, May 1999
- Lang, Lixin; Jagoda, Elaine; Schmall, Bernard
- Journal of Medicinal Chemistry, Vol. 42, Issue 9
In vivo Measurement of the Serotonin Transporter with (S)-([18F]fluoromethyl)-(+)-McN5652
journal, June 2003
- Brust, P.; Hinz, R.; Kuwabara, H.
- Neuropsychopharmacology, Vol. 28, Issue 11