Universität zu Köln

Willmann, Michael, Hegger, Julian, Neumaier, Bernd and Ermert, Johannes (2021). Radiosynthesis and Biological Evaluation of [F-18]R91150, a Selective 5-HT2A Receptor Antagonist for PET-Imaging. ACS Med. Chem. Lett., 12 (5). S. 738 - 745. WASHINGTON: AMER CHEMICAL SOC. ISSN 1948-5875

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Abstract

Serotonergic 5-HT2A receptors in cortical and forebrain regions are an important substrate for the neuromodulatory actions of serotonin in the brain. They have been implicated in the etiology of many neuropsychiatric disorders and serve as a target for antipsychotic, antidepressant, and anxiolytic drugs. Positron emission tomography imaging using suitable radioligands can be applied for in vivo quantification of receptor densities and receptor occupancy for therapy evaluation. Recently, the radiosynthesis of the selective 5-HT2AR antagonist [F-18]R91150 was reported. However, the six-step radiosynthesis is cumbersome and time-consuming with low radiochemical yields (RCYs) of <5%. In this work, [F-18]R91150 was prepared using late-stage Cu-mediated radiofluorination to simplify its synthesis. The detailed protocol enabled us to obtain RCYs of 14 +/- 1%, and the total synthesis time was reduced to 60 min. In addition, autoradiographic studies with [F-18]R91150 in rat brain slices revealed the typical uptake pattern of 5-HT2A receptor ligands.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Willmann, Michael UNSPECIFIED UNSPECIFIED UNSPECIFIED Hegger, Julian UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Bernd UNSPECIFIED UNSPECIFIED UNSPECIFIED Ermert, Johannes UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-576279
DOI:	10.1021/acsmedchemlett.0c00658
Journal or Publication Title:	ACS Med. Chem. Lett.
Volume:	12
Number:	5
Page Range:	S. 738 - 745
Date:	2021
Publisher:	AMER CHEMICAL SOC
Place of Publication:	WASHINGTON
ISSN:	1948-5875
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language SEROTONIN RECEPTORS; IN-VIVO; RAT-BRAIN; LIGAND I-123-R91150; EMISSION-TOMOGRAPHY; HEALTHY-VOLUNTEERS; BINDING; VALIDATION; EXPRESSION; F-18 Multiple languages Chemistry, Medicinal Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/57627