Indian Journal of Nuclear Medicine
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ORIGINAL ARTICLE
Year : 2016  |  Volume : 31  |  Issue : 4  |  Page : 267-273

Preparation and preclinical evaluation of 68Ga-DOTA-amlodipine for L-type calcium channel imaging


1 Nuclear Medicine and Molecular Imaging Research Center, Shiraz University of Medical Science, Shiraz, Iran
2 Department of Medicinal Chemistry, Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, Iran
3 Department of Medicinal Chemistry, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran

Correspondence Address:
Amir Reza Jalilian
Radiation Application Research School, Nuclear Science and Technology Research Institute, P.O. Box: 14395-836, Tehran
Iran
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0972-3919.190797

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Aim: In order to develop a possible tracer for L-type calcium channel imaging, we here report the development of a Ga-68 amlodipine derivative for possible PET imaging. Materials and Methods: Amlodipine DOTA conjugate was synthesized, characterized and went through calcium channel blockade, toxicity, apoptosis/necrosis tests. [68Ga] DOTA AMLO was prepared at optimized conditions followed by stability tests, partition coefficient determination and biodistribution studies using tissue counting and co incidence imaging up to 2 h. Results: [68Ga] DOTA AMLO was prepared at pH 4–5 in 7–10 min at 95°C in high radiochemical purity (>99%, radio thin layer chromatography; specific activity: 1.9–2.1 GBq/mmol) and was stable up to 4 h with a log P of −0.94. Calcium channel rich tissues including myocardium, and tissues with smooth muscle cells such as colon, intestine, and lungs demonstrated significant uptake. Co incidence images supported the biodistribution data up to 2 h. Conclusions: The complex can be a candidate for further positron emission tomography imaging for L type calcium channels.


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