3-Iodothyronamine increases transient receptor potential melastatin channel 8 (TRPM8) activity in immortalized human corneal epithelial cells

Upregulation of Transient Receptor Potential Vanilloid Type-1 Channel Activity and Ca2+Influx Dysfunction in Human Pterygial Cells

“…45 Similarly, TRPM8 expression may contribute to the pterygial transition, as this channel plays a role in cancer diseases concerning by modulating proliferation and cell cycle progression. 55 Notably, TRPM8 is functionally expressed at higher levels in hPtEC (data not shown) compared with human corneal epithelial cells and conjunctival epithelial cells, 41,56 whereas TRPM8 mRNA expression was not significantly different (Fig. 2).…”

“…Such a strategy is tenable, as TRPM8 activation by a thyroid hormone analogue (3-T 1 AM) inhibited through crosstalk CAP-and hypertonic-induced increases in TRPV1 channel activity in both HCjEC and HCEC. 41,56 …”

Trace Amines and Their Receptors

“…This has subsequently been verified by numerous laboratories (Mühlhaus et al, 2014;Cöster et al, 2015;Chiellini et al, 2017), with 3IT also shown to act as an agonist at TAAR2 (Babusyte et al, 2013;Cichero and Tonelli, 2017) and as an inverse agonist at TAAR5 (Dinter et al, 2015c). 3IT is promiscuous, however, and also interacts with high affinity at a 2 -adrenoceptors (Regard et al, 2007;Dinter et al, 2015b), b-adrenergic receptors (Meyer and Hesch, 1983;Kleinau et al, 2011;Dinter et al, 2015a), muscarinic acetylcholine receptors (Laurino et al, 2016), transient receptor potential cation channel subfamily M member 8 ion channels (Khajavi et al, 2015;Lucius et al, 2016), various monoamine and organic anion transporters (Snead et al, 2007;Panas et al, 2010), and molecular target(s) within mitochondria, including the F 1 -F 0 ATP synthase (Cumero et al, 2012) and possibly complex III (Venditti et al, 2011). 3IT also tightly binds to the plasma protein apolipoprotein B-100 .…”

The impact of scopolamine pretreatment on 3-iodothyronamine (T1AM) effects on memory and pain in mice

“…However, also T1AM has a complex pharmacodynamic profile, being considered a multi-target molecule since amine interaction at several Gprotein-coupled receptors including trace amine-associated receptors (TAAR1 and 8; Scanlan et al, 2004;Mühlhaus et al, 2014), α2 (Regard et al, 2007;Dinter et al 2015a), β2 adrenoreceptors (Dinter et al, 2015b) and ion channels (Lucius et al, 2015) have been reported. Until now, none of these targets has been recognized to be involved in the behavioral effects of low T1AM doses, including memory stimulation and hyperalgesia.…”