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Discovery and evaluation of a novel ^(18)F-labeled vasopressin 1a receptor PET ligand with peripheral binding specificity
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作者 junqi hu Yinlong Li +11 位作者 Chenchen Dong huiyi Wei Kai Liao Junjie Wei Chunyu Zhao Ahmad Chaudhary Jiahui Chen Hao Xu Ke Zhong Steven H.Liang Lu Wang Weijian Ye 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2024年第9期4014-4027,共14页
The arginine-vasopressin(AVP)hormone plays a pivotal role in regulating various physiological processes,such as hormone secretion,cardiovascular modulation,and social behavior.Recent studies have highlighted the V1a r... The arginine-vasopressin(AVP)hormone plays a pivotal role in regulating various physiological processes,such as hormone secretion,cardiovascular modulation,and social behavior.Recent studies have highlighted the V1a receptor as a promising therapeutic target.In-depth insights into V1a receptor-related pathologies,attained through in vivo imaging and quantification in both peripheral organs and the central nervous system(CNS),could significantly advance the development of effective V1a inhibitors.To address this need,we develop a novel V1a-targeted positron emission tomography(PET)ligand,[^(18)F]V1A-2303([^(18)F]8),which demonstrates favorable in vitro binding affinity and selectivity for the V1a receptor.Specific tracer binding in peripheral tissues was also confirmed through rigorous cell uptake studies,autoradiography,biodistribution assessments.Furthermore,[^(18)F]8 was employed in PET imaging and arterial blood sampling studies in healthy rhesus monkeys to assess its brain permeability and specificity,whole-body distribution,and kinetic properties.Our research indicated[^(18)F]8 as a valuable tool for noninvasively studying V1a receptors in peripheral organs,and as a foundational element for the development of next-generation,brain-penetrant ligands specifically designed for the CNS. 展开更多
关键词 VASOPRESSIN AUTISM V1a receptor Positron emission tomography PET imaging RADIOLABELING Fluorine 18 Kinetic modeling
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Global Well-Posedness of the BCL System with Viscosity 被引量:1
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作者 junqi hu 《Chinese Annals of Mathematics,Series B》 SCIE CSCD 2009年第2期153-172,共20页
The BCL system, a kind of equations governing the motion of the free surface of water waves in R3, is studied. Some results on the global existence, uniqueness and regularity of solutions to such system with small ini... The BCL system, a kind of equations governing the motion of the free surface of water waves in R3, is studied. Some results on the global existence, uniqueness and regularity of solutions to such system with small initial data are obtained. 展开更多
关键词 Pseudo-differential operator Water waves Global well-posedness
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