1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1H-INDOL-2-ONE

Galanin-3 receptor

HT-2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK ^- cells expressing the human Gal ₃ receptor (K _i =17.44±0.01 nM; n>100) and is highly selective for Gal ₃ over the Gal ₁ and Gal ₂ subtypes (K _i >10,000 nM for each subtype; n=46 of each subtype). When tested for the antagonism of galanin-evoked inhibition of adenylyl cyclase, HT-2157 (0.1-10 μM) produces concentration-dependent rightward shifts of the concentration-effect curve to galanin.

The galanin-3 receptor antagonist, HT-2157 (SNAP 37889), reduces operant responding for ethanol in alcohol-preferring rats. The novel selective GALR3 antagonist, HT-2157, to reduce anxiety-like behaviour and voluntary ethanol consumption in the iP (alcohol-preferring) rat. Male iP rats treated with HT-2157 at a dose of 30 mg/kg (i.p.) do not show altered locomotor activity or changes in anxiety-like behaviour in the elevated plus maze or light-dark paradigms. Treatment with HT-2157 (30 mg/kg, i.p.) reduces operant responding for solutions containing ethanol, sucrose and saccharin. Collectively, results from the current study shows that HT-2157 (30 mg/kg, i.p.) is effective in reducing operant responding for ethanol, independent of a sedative effect.