FFN-102 (trifluoroacetate salt)

FFN-102 is a fluorescent false neurotransmitter (FFN) that is a substrate for the dopamine transporter (DAT) and vesicular monoamine transporter 2 (VMAT2).¹ It is a pH-dependent fluorescent probe that labels dopamine cell bodies, axons, and presynaptic terminals. It can also be used to monitor dopamine exocytosis.² It has a pK_a of 6.2 and displays pH-dependent excitation spectra of 340 and 370 nm at pH 5 and 7.4, respectively, which correspond to vesicular and cytoplasmic pH values.¹ The emission spectrum of FFN-102 is pH-independent at 453 nm, but the intensity of emission is pH-dependent with a higher intensity at a pH of 7.4. FFN-102 inhibits DAT (13.6% at a concentration of 10 µM) and the serotonin (5-HT) receptor subtype 5-HT_2c (K_i = ~3 µM) but does not bind to 37 other central nervous system receptors and transporters, including dopamine receptors, up to a concentration of 10 µM.¹

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1. Rodriguez, P.C., Pereira, D.B., Borgkvist, A., et al. Fluorescent dopamine tracer resolves individual dopaminergic synapses and their activity in the brain. Proc. Natl. Acad. Sci. USA 110(3), 870-875 (2013).

2. Liu, X., Savy, A., Maurin, S., et al. A dual functional electroactive and fluorescent probe for coupled measurements of vesicular exocytosis with high spatial and temporal resolution. Agnew. Chem. Int. Ed. Engl. 56(9), 2366-2370 (2017).