Radiosynthesis of β-phenylethylamine derivatives for cardiac sympathetic nervous PET imaging
- 52 Downloads
β-Phenylethylamine is one of the core structure for synthesis of cardiac imaging agents. 11C-MDA is a β-phenylethylamine-based agent, which showed potential imaging performance. To further explore the potentials of the β-phenylethylamine derivatives, 11C-MPEA, 11C-m-MTyr and 11C-p-MTyr were synthesized. The three agents were stable in vitro. The radioactivity uptake of them in myocardium was similar to that in muscle. 11C-p-MTyr PET/CT imaging in New Zealand white rabbits showed a blurred left ventricular image along with a reduced radioactivity uptake. These results suggested the newly synthesized β-phenylethylamine derivatives, unlike 11C-MDA, may not be suitable as the cardiac PET imaging agents.
Keywordsβ-Phenylethylamine Carbon-11 labeling Cardiac sympathetic nervous Positron imaging agent
This work was supported in part by a grant from National Natural Science Foundation of China (81660295) and Natural Science Foundation of Inner Mongolia (2016MS(LH)0812).
YH wrote the paper and performed the experiments. XZ performed the experiments for drug synthesis. JL performed the experiments for biological distribution experiment. JZ conceived and designed the experiments. XW analyzed the data of PET imaging.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no conflict of interest.
- 4.Ekas RD Jr, Steenberg ML, Lokhandwala MF (1983) Increased norepinephrine release during sympathetic nerve stimulation and its inhibition by adenosine in the isolated perfused kidney of spontaneously hypertensive rats. Clin Exp Hypertens 1:41–48Google Scholar
- 9.Rijnierse MT, Allaart CP, de Haan S, Harms HJ, Huisman MC, Wu L, Beek AM, Lammertsma AA, van Rossum AC, Knaapen P (2015) Sympathetic denervation is associated with microvascular dysfunction in non-infarcted myocardium in patients with cardiomyopathy. Eur Heart J Cardiovasc Imaging 7:788–798CrossRefGoogle Scholar
- 11.Eskola O, Grönroos T, Bergman J, Haaparanta M, Marjamäki P, Lehikoinen P, Forsback S, Langer O, Hinnen F, Dollé F, Halldin C, Solin O (2004) A novel electrophilic synthesis and evaluation of medium specific radioactivity (1R,2S)-4-18F-fluorometaraminol, a tracer for the assessment of cardiac sympathetic nerve integrity with PET. Nucl Med Biol 1:103–110CrossRefGoogle Scholar
- 12.Nguyen NT, Degrado TR, Chakraborty P, Wieland DM, Schwaiger M (1997) Myocardial kinetics of carbon-11-epinephrine in the isolated working rat heart. J Nucl Med 5:780–785Google Scholar