Synthesis and evaluation of new radioligands [11C]A-833834 and [11C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors
Andrew G. Horti,Hayden T. Ravert,Yongjun Gao,Daniel P. Holt,William H. Bunnelle,Michael R. Schrimpf,Tao Li,Jianguo Ji,Heather Valentine,Ursula Scheffel,Hiroto Kuwabara,Dean F. Wong,Robert F. Dannals +12 more
TLDR
Low specific α7-nAChR binding in the mouse brain is low due to the insufficient binding affinity of the radioligand, while the very high binding affinity A-833834 and A-752274 exhibited good specificbinding in the α 7-n aChR-rich mouse brain regions.About:
This article is published in Nuclear Medicine and Biology.The article was published on 2013-04-01 and is currently open access. It has received 19 citations till now. The article focuses on the topics: Radioligand.read more
Citations
More filters
Journal ArticleDOI
Evaluating the role of the alpha-7 nicotinic acetylcholine receptor in the pathophysiology and treatment of schizophrenia
Jared W. Young,Mark A. Geyer +1 more
TL;DR: The accumulating evidence is positive, but more work is required using positron emission tomography to understand current alterations in α7 nAChR expression and their relationship to symptoms, and cross-species behavioral tasks should be used more regularly to determine the predictive efficacy of treatments.
Journal ArticleDOI
Therapeutic Potential of α7 Nicotinic Acetylcholine Receptors
TL;DR: The aim of this review is to discuss the current knowledge of α7 nAChRs and their relevance as a target in specific functional systems and disease states.
Journal ArticleDOI
Human brain imaging of α7 nAChR with [(18)F]ASEM: a new PET radiotracer for neuropsychiatry and determination of drug occupancy.
Dean F. Wong,Hiroto Kuwabara,Martin G. Pomper,Daniel P. Holt,James Robert Brašić,Noble George,Boris Frolov,William Willis,Yongjun Gao,Heather Valentine,Ayon Nandi,Lorena Gapasin,Robert F. Dannals,Andrew G. Horti +13 more
TL;DR: The characteristics of [18F]ASEM are consistent with the ability to quantify α7-nAChR in the human brain and is suitable for imaging neuropsychiatric disorders and target engagement (receptor occupancy) of potential α 7-n AChR drugs.
Journal ArticleDOI
Derivatives of dibenzothiophene for positron emission tomography imaging of α7-nicotinic acetylcholine receptors.
Yongjun Gao,Kenneth J. Kellar,Robert P. Yasuda,Thao Tran,Yingxian Xiao,Robert F. Dannals,Andrew G. Horti +6 more
TL;DR: A new series of derivatives of 3-(1,4-diazabicyclo[3.2.2]nonan-4-yl)dibenzo[b,d]thiophene 5,5-dioxide with high binding affinities and selectivity for α7-nicotinic acetylcholine receptors (α7-nAChRs) has been synthesized for positron emission tomography (PET) imaging of α7
Journal ArticleDOI
18F-ASEM, a Radiolabeled Antagonist for Imaging the α7-Nicotinic Acetylcholine Receptor with PET
Andrew G. Horti,Yongjun Gao,Hiroto Kuwabara,Yuchuan Wang,Sofya Abazyan,Robert P. Yasuda,Thao Tran,Yingxian Xiao,Niaz Sahibzada,Daniel P. Holt,Kenneth J. Kellar,Mikhail V. Pletnikov,Martin G. Pomper,Dean F. Wong,Robert F. Dannals +14 more
TL;DR: 18F-ASEM holds promise as a radiotracer with suitable imaging properties for quantification of α7-nAChR in the human brain, which is in agreement with previous postmortem human data.
References
More filters
Journal ArticleDOI
Mammalian nicotinic acetylcholine receptors: from structure to function.
TL;DR: This review provides a comprehensive overview of the advancement of functional and genetic studies in the late 1980s and the more recent revelations of the impact that the rich diversity in function and expression of this receptor family has on neuronal and nonneuronal cells throughout the body.
Journal ArticleDOI
Neuronal nicotinic receptors: from structure to pathology
Cecilia Gotti,Francesco Clementi +1 more
TL;DR: This review will attempt to survey the major achievements reached in the study of the structure and function of NAChRs by examining their regional and cellular localisation and the molecular basis of their functional diversity mainly in pharmacological and biochemical terms.
Journal ArticleDOI
Brain nicotinic acetylcholine receptors : native subtypes and their relevance
TL;DR: The increasing knowledge of subtype composition and roles will be of considerable interest for the development of new and clinically useful nicotinic acetylcholine receptor ligands.
Journal ArticleDOI
β-Amyloid1–42 Binds to α7 Nicotinic Acetylcholine Receptor with High Affinity IMPLICATIONS FOR ALZHEIMER'S DISEASE PATHOLOGY
Hoau-Yan Wang,Daniel H. S. Lee,Michael R. D'Andrea,Per A. Peterson,Richard P. Shank,Allen B. Reitz +5 more
TL;DR: It is proposed that interaction of the α7nAChR and Aβ1–42 is a pivotal mechanism involved in the pathophysiology of Alzheimer's disease.
Journal ArticleDOI
Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia.
Ann Olincy,Josette G. Harris,Lynn Johnson,Vicki Pender,Susan Kongs,Diana Allensworth,Jamey Ellis,Gary O. Zerbe,Sherry Leonard,Karen E. Stevens,James O. Stevens,Laura F. Martin,Lawrence E. Adler,Ferenc Soti,William R. Kem,Robert Freedman +15 more
TL;DR: An alpha7 nicotinic agonist appears to have positive effects on neurocognition in persons with schizophrenia, and significant neurocognitive improvement was found on the Repeatable Battery for the Assessment of Neuropsychological Status total scale score.