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Pharmacological modulation of the transient receptor potential melastatin type 8 (TRPM8) is currently under investigation as a new approach mainly for the treatment of pain. In this study, a series of N-substituted tryptamines was prepared to explore the structural requirements determining TRPM8 modulation. As a result of a fluorescence-based screening assay, we identified two compounds acting as an activator (2-(1H-indol-3-yl)-N-(4-phenoxybenzyl) ethanamine, compound 21) or an inhibitor (N,N-dibenzyl-2-(1H-indol-3-yl) ethanamine, compound 12) of calcium influx in HEK293 cells. In patch-clamp recordings, compound 21 displayed a significantly higher potency (EC 50 = 40±4 µM) and a similar efficacy when compared to menthol; by contrast, compound 12 produced a concentrationdependent inhibition of menthol-induced TRPM8 currents (IC 50 = 367±24 nM). Molecular modelling studies using a homology model of a single TRPM8 subunit identified a putative binding site located between the VSD and the TRP box, disclosing two different binding modes for the agonist and the antagonist.

The cultivar per se (genotype) behaved as the most influencing factor conditioning pomegranate sugar and organic acids profiles, antioxidant activity, and total phenolics. Given the divergence observed on bioactive compounds concentrations and antioxidant activity among evaluated cultivars, the genotype factor should be considered as the most influencing factor in future breeding programs to enhance the synthesis of beneficial bioactive compounds.

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Regarding physical, chemical and volatile composition and sensory properties, very-early apricot cultivars could be recommended for fresh consumption. However, future research must be focused on increasing their contents of sugars, organic acids and bioactive and volatile compounds, perhaps via cultural practices such as deficit irrigation and/or mulching.

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