The purpose of this research is to use specialized brain imaging techniques, Positron Emission Tomography (PET) scan and Magnetic Resonance Imaging (MRI), to learn more about the brain chemistry, e.g., how neurotransmitters and receptors in the brain function in people with schizophrenia compared to healthy controls.

Start Date18 Aug 2022

Sponsor / Collaborator

Washington University School of Medicine

NCT04055467 / CompletedPhase 1IIT

Brain Imaging of Nicotinic Acetylcholine Receptors in Tobacco Users and Nonusers

The proposed study will help fill gaps in existing research by determining if nicotine-dependent cigarette smokers show changes in α7 nicotinic acetylcholine receptor (nAChR) availability when compared to matched historical controls using positron emission tomography (PET) imaging and the radioactive ligand [18F]-ASEM (3-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-6 [18F]fluorodibenzo[b,d]thiophene 5,5-dioxide), an α7 nAChR antagonist. The study will also explore whether α7 nAChR availability influences clinically relevant measures of tobacco abstinence (e.g., withdrawal and craving, cognitive impairment), self-reported cigarettes per day, and time to relapse during an 8-day quit attempt during which smokers can receive escalating payments contingent upon providing objective evidence (breath CO and urinary cotinine) of smoking abstinence.

Start Date16 Dec 2019

Sponsor / Collaborator

The Johns Hopkins University

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100 Clinical Results associated with [18F]ASEM

100 Translational Medicine associated with [18F]ASEM

100 Patents (Medical) associated with [18F]ASEM

Literatures (Medical) associated with [18F]ASEM

01 Jun 2017·European Journal of Nuclear Medicine and Molecular ImagingQ1 · MEDICINE

PET imaging of α7 nicotinic acetylcholine receptors: a comparative study of [18F]ASEM and [18F]DBT-10 in nonhuman primates, and further evaluation of [18F]ASEM in humans

Q1 · MEDICINE

Article

Author: Holden, Daniel ; Nabulsi, Nabeel ; Brust, Peter ; Ropchan, Jim ; Li, Songye ; Scheunemann, Matthias ; Teodoro, Rodrigo ; Zheng, Ming-Qiang ; Labaree, David ; Hillmer, Ansel T ; Huang, Yiyun ; Esterlis, Irina ; Cosgrove, Kelly P ; Carson, Richard E ; Lin, Shu-Fei ; Pracitto, Richard ; Deuther-Conrad, Winnie

PURPOSEThe α₇ nicotinic acetylcholine receptor (nAChR) is implicated in many neuropsychiatric disorders, making it an important target for positron emission tomography (PET) imaging. The first aim of this work was to compare two α₇ nAChRs PET radioligands, [¹⁸F]ASEM (3-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-6-([¹⁸F]fluorodibenzo[b,d]thiophene 5,5-dioxide) and [¹⁸F]DBT-10 (7-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-2-([¹⁸F]fluorodibenzo[b,d]thiophene 5,5-dioxide), in nonhuman primates. The second aim was to assess further the quantification and test-retest variability of [¹⁸F]ASEM in humans.METHODSPET scans with high specific activity [¹⁸F]ASEM or [¹⁸F]DBT-10 were acquired in three rhesus monkeys (one male, two female), and the kinetic properties of these radiotracers were compared. Additional [¹⁸F]ASEM PET scans with blocking doses of nicotine, varenicline, and cold ASEM were acquired separately in two animals. Next, six human subjects (five male, one female) were imaged with [¹⁸F]ASEM PET for 180 min, and arterial sampling was used to measure the parent input function. Different modeling approaches were compared to identify the optimal analysis method and scan duration for quantification of [¹⁸F]ASEM distribution volume (V _T). In addition, retest scans were acquired in four subjects (three male, one female), and the test-retest variability of V _T was assessed.RESULTSIn the rhesus monkey brain [¹⁸F]ASEM and [¹⁸F]DBT-10 exhibited highly similar kinetic profiles. Dose-dependent blockade of [¹⁸F]ASEM binding was observed, while administration of either nicotine or varenicline did not change [¹⁸F]ASEM V _T. [¹⁸F]ASEM was selected for further validation because it has been used in humans. Accurate quantification of [¹⁸F]ASEM V _T in humans was achieved using multilinear analysis with at least 90 min of data acquisition, resulting in V _T values ranging from 19.6 ± 2.5 mL/cm³ in cerebellum to 25.9 ± 2.9 mL/cm³ in thalamus. Test-retest variability of V _T was 11.7 ± 9.8%.CONCLUSIONSThese results confirm [¹⁸F]ASEM as a suitable radiotracer for the imaging and quantification of α₇ nAChRs in humans.

01 Apr 2015·Journal of Labelled Compounds and RadiopharmaceuticalsQ4 · MEDICINE

Microwave radiosynthesis of [¹⁸F]ASEM, anα7-nAChR antagonist

Q4 · MEDICINE

Article

Author: Horti, Andrew G. ; Gao, Yongjun ; Holt, Daniel P. ; Ravert, Hayden T. ; Dannals, Robert F.

An improvement of the original radiochemical synthesis of [(18) F]ASEM, an α7-nicotinic acetylcholinergic receptor radioligand, is reported. The new procedure utilizes microwave-assisted radiofluorination. In addition, a new preparative HPLC method was developed to eliminate a chemical impurity in the final product. Quality control procedures were also enhanced to improve detection of product with enhanced resolution of potential impurities. [(18) F]ASEM was produced in 20.1 ± 8.9% non-decay corrected (NDC) yield with an average synthesis time of 57 min and an average specific radioactivity of 856 ± 332 GBq/µmol (23 ± 9 Ci/µmol).

100 Deals associated with [18F]ASEM

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Indication	Highest Phase	Country/Location	Organization	Date
Schizophrenia	Phase 1	US	Washington University School of Medicine	18 Aug 2022
Tobacco Use Disorder	Phase 1	US	National Institute on Drug Abuse	16 Dec 2019
Diagnostic agents	Phase 1	-	The Johns Hopkins University School of Medicine	-
Diagnostic agents	Phase 1	-	Georgetown University in Qatar	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04055467 (CTgov)	Phase 1	Tobacco Use Disorder	15	Contingency Management+[F18]-ASEM (3-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-6-[18F]fluorodibenzo[b,d]thiophene 5,5-dioxide)	arnriigbxe(nmabdxskyz) = prgudtifmf csqtgdften (ysgahfcajq, wjhiexrkel - inqaartekv) View more	-	06 Aug 2024

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