Compositions and methods related to serotonin 5-HT1A receptors

Details Compositions and methods related to serotonin 5-HT1A receptors Compositions and methods related to serotonin 5-HT1A receptors

2007-01-24

2010-06-08

Wilson, James O (Department: 1624)

Drug, bio-affecting and body treating compositions

In vivo diagnosis or in vivo testing

X-ray contrast imaging agent

C514S252120, C544S358000

Reexamination Certificate

active

07731940

ABSTRACT:
Contemplated substituted arylpiperazinyl compounds, and most preferably18F-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 with18F-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.

REFERENCES:
patent: 6670400 (2003-12-01), Bigg et al.
patent: 6821981 (2004-11-01), Stack et al.
patent: 6831084 (2004-12-01), Childers, Jr. et al.
patent: 6861427 (2005-03-01), Stack et al.
patent: 94/19026 (1994-09-01), None
patent: 96/01656 (1996-01-01), None
Wong et al. Emerging Therapeutic Targets, 1999, 3(4), 571-586.
Grigoriadis .xpert Opinion on Therapeutic Targets, 2003, 9 (4), 651-84.
Green et al. Drug Discovery Today, 2006, 11 (15/16), 681-693.
Langstrom et al. Acta Chimica Scandinavica, 1999, 53, 651-69.
Bailey et al (editors of Positron Emission Tomography, published 2005, chapter 6, pp. 127-159, and chapter 9, pp. 203-222.
“Neurodegenerative diseases”, http://www.nlm.nih.gov/cgi/mesh/2008/MB—cgi, accessed Dec. 8, 2008, attached as PDF.
“Movement Disorders”, http://www.nlm.nih.gov/cgi/mesh/2009/MB—cgi?mode=&index=8693&field=all&HM=&II=&PA=&form=&input=, accessed Jul. 13, 2009, attached as PDF.
Lang et al. Journal of Medicinal Chemistry, 1999, 42, 1576-86.
Saigal, et al., Synthesis and Biologic Evaluation of a Novel Serotonin 5-HT Receptor Radioligand, F-Labeled Mefway, in Rodents and Imaging by PET in a Nonhuman Primate, Journal of Nuclear Medicine, Oct. 2006, pp. 1697-1706, vol. 47 No. 10, Society of Nuclear Medicine.
Kepe, et al., Serotonin 1A Receptors in the Living Brain of Alzheimer's Disease Patients, Proceedings of the National Academy of Science of the US, Jan. 9, 2006, pp. 702-707, issue 103, PNAS 2006, online.
Brust, et al., in vivo Measurements of the Serotonin Transporter with (S)-([18F]fluoromethyl)-(+)-McN5652, Neuropsychopharmacology, 2003, pp. 2010-2019, vol. 28, Nature Publishing Group, online.
Cliffe, A Retrospect on the Discovery of Way-100635 and the Prospect for Improved 5-HT1a Receptor PET Radioligands, Nuclear Medicine & Biology, Apr. 2000, pp. 441-447, vol. 27, Elsevier Science Inc.

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