A convenient and efficient solid phase extraction-based pathway for purification of melanin-targeted probe 18F-P3BZA

Hong, Zheng-Yuan; Yu, Biao; Xiao, Jiachao; Feng, Hongyan; Ma, Xiaowei; Cheng, Zhen; Bu, Lihong

doi:10.1016/j.microc.2021.106008

Cited by 3 publications

(1 citation statement)

References 12 publications

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“…Radiosynthesis and characterization of 18 F-P3BZA was performed as previously described [18,20]. 18 F-P3BZA was puri ed via an improved solid phase extraction-based method as previously reported [21].…”

Section: Preparation Of 18 F-p3bzamentioning

confidence: 99%

Neuromelanin-Targeted 18F-P3BZA PET/MR Imaging of the Substantia Nigra in Rhesus Macaques

Feng,

Tu,

Wang

et al. 2024

Preprint

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Background Neuromelanin is mostly located in dopaminergic neurons in the substantia nigra (SN) pars compacta, and can be detected by magnetic resonance imaging (MRI). It is a promising biomarker for Parkinson’s disease imaging. We previously developed N-(2-(diethylamino)-ethyl)-18F-5-fluoropicolinamide (18F-P3BZA) as a potential melanin-specific probe for detection of melanoma in living humans. In the current study we investigated whether 18F-P3BZA could be used to quantitatively detect neuromelanin in the SN in healthy rhesus macaques. Results 18F-P3BZA exhibited desired hydrophobicity with estimated log Know 5.08 and log D7.4 1.68. 18F-P3BZA accumulated specifically in neuromelanotic PC12 cells, melanin-rich melanoma cells, and melanoma xenografts. 18F-P3BZA readily crossed the blood-brain barrier with brain transport coefficients (Kin) of 40 ± 8 µL g-1s-1. PET/MRI 18F-P3BZA provided clear visualization of neuromelanin-rich SN at 30–60 min after injection in healthy macaques. In in vitro autoradiography studies 18F-P3BZA exhibited high levels of binding to the SN, and almost no binding to surrounding midbrain tissues. Conclusion 18F-P3BZA PET/MRI clearly images neuromelanin in the SN, and may assist in the diagnosis of neurological diseases associated with abnormal neuromelanin expression such as Parkinson’s disease.

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Section: Preparation Of 18 F-p3bzamentioning

confidence: 99%