SNAP-37889

A potent, selective galanin-3 receptor (Gal3) antagonist with Ki of 17.44 nM, displays highly selective for Gal3 over the Gal1 and Gal2 subtypes (both Ki >10 uM) ; attenuates stress-induced hyperthermia in mice, partially antagonizes the galanin-evoked reduction in hippocampal serotonin, exhibits anxiolytic- and antidepressant-like profiles in vivo.Depression Phase 2 Clinical (In Vitro) :HT-2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK- cells expressing the human Gal3 receptor (Ki=17.44±0.01 nM; n>100) and is highly selective for Gal3 over the Gal1 and Gal2 subtypes (Ki>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. (In Vivo) :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.

303149-14-6

HT-2157 | HT2157 | HT 2157 | SNAP37889 | SNAP 37889

Neuroscience

>98% (HPLC)

DMSO: ≥ 29 mg/mL

O=C1N (C2=CC=CC=C2) C3=C (C=CC=C3) /C1=N/C4=CC=CC (C (F) (F) F) =C4

C21H13F3N2O

366.3359

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.