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Discovery and evaluation of a novel 18F-labeled vasopressin 1a receptor PET ligand with peripheral binding specificity

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ACTA PHARMACEUTICA SINICA B 2024年第9期14卷 4014-4027页

作者： Hu, Junqi Li, Yinlong Dong, Chenchen Wei, Huiyi Liao, Kai Wei, Junjie Zhao, Chunyu Chaudhary, Ahmad Chen, Jiahui Xu, Hao Zhong, Ke Liang, Steven H. Wang, Lu Ye, Weijian Jinan Univ Affiliated Hosp 1 Ctr Cyclotron & PET Radiopharmaceut Dept Nucl Med Guangzhou 510630 Peoples R China Jinan Univ Affiliated Hosp 1 Key Lab Basic & Translat Res Radiopharmaceut Guangzhou 510630 Peoples R China Emory Univ Dept Radiol & Imaging Sci Atlanta GA 30322 USA Sun Yat Sen Univ Sun Yat Sen Mem Hosp Dept Pharm Guangzhou 510120 Peoples R China

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, [F-18]V1A-2303 ([F-18]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, [F-18]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 [F-18]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.

关键词： vasopressin Autism V1a receptor Positron emission tomography PET imaging Radiolabeling Fluorine 18 Kinetic modeling arginine-vasopressin SOCIAL RECOGNITION SEX-DIFFERENCES AVPR1A GENE AUTISM V1A ASSOCIATION ANTAGONIST OXYTOCIN POTENT

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Tolvaptan attenuated brain edema in experimental intracerebral hemorrhage

Tolvaptan attenuated brain edema in experimental intracerebr...

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第十四届中国医师协会神经外科医师年会

作者： Qiang Tan Yuhan Li Peiwen Guo Jiru Zhou Zhouyang Jiang Xin Liu Zhi Chen Hua Feng Department of Neurosurgery Southwest HospitalThird Military Medical UniversityArmy Medical University State Key Laboratory Of Silkworm Genome Biology Southwest University

arginine-vasopressin（AVP） is believed to be positively correlated with the brain edema formation, but the underlying mechanism is still unclear. In this study, we explored the role of the V2 receptors antagonist tolvaptan on brain edema following intracerebral hemorrhage（ICH） with a rat model. Animals were randomly given tolvaptan or vehicle through oral gavage at 12 h, 36 h, and 60 h after ICH surgery. Brain swelling（%）,brain water content（BWC）, neurological scores, Evans blue fluorescence and blood-brain barrier（BBB） tight junction proteins were measured to evaluate the effect of tolvaptan in ICH. We found that tolvaptan alleviated the brain swelling（%）, decreased the BWC growth, and attenuated the neurological deficits after ICH（p ＜ 0.05,vs vehicle）. What’s more, tolvaptan increased the expression of ZO-1 and occludin（p ＜ 0.05, vs vehicle）, which might be attributed to the down-regulated effects of tolvaptan on MMP-9. These results provided evidence supporting the use of tolvaptan for ICH-induced brain edema. Large animal experiments are required to further explore the efficacy and mechanism of tolvaptan in ICH treatment.

关键词： Brain edema arginine-vasopressin V1 receptors V2 receptors Tolvaptan Blood brain barrier

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