HT-2157

HT-2157 is an antagonist of the galanin-3 receptor (GAL₃; K_i = 17 nM).¹ It is selective for GAL₃ over GAL₁ and GAL₂ (K_is = >10 µM for both). HT-2157 (10 µM) induces apoptosis in various cell types, including HL-60 leukemia and BV-2 murine microglial cells, as well as isolated human peripheral blood mononuclear cells (PBMCs).² It decreases operant alcohol, sucrose, and saccharin self-administration in rats when administered at a dose of 30 mg/kg.³ HT-2157 (3 and 10 mg/kg) increases drinking in the Vogel punished drinking task and reduces immobility time in the forced swim test in rats, indicating anxiolytic- and antidepressant-like activities, respectively.⁴

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1. Konkel, M.J., Lagu, B., Boteju, L.W., et al. 3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists. J. Med. Chem. 49(13), 3757-3758 (2006).

2. Koller, A., Rid, R., Beyreis, M., et al. In vitro toxicity of the galanin receptor 3 antagonist SNAP 37889. Neuropeptides 56, 83-88 (2016).

3. Ash, B.L., Zanatta, S.D., Williams, S.J., et al. The galanin-3 receptor antagonist, SNAP 37889, reduces operant responding for ethanol in alcohol-preferring rats. Regul. Pept. 166(1-3), 59-67 (2011).

4. Swanson, C.J., Blackburn, T.P., Zhang, X., et al. Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc. Natl. Acad. Sci. USA 102(48), 17489-17494 (2005).