Molecular Formula | C21H13F3N2O |
Molar Mass | 366.34 |
Density | 1.29±0.1 g/cm3(Predicted) |
Melting Point | 141-144 °C |
Boling Point | 484.0±55.0 °C(Predicted) |
Solubility | DMSO: ≥ 29 mg/mL |
pKa | -0.36±0.20(Predicted) |
Storage Condition | -20℃ |
In vitro study | 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. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.73 ml | 13.649 ml | 27.297 ml |
5 mM | 0.546 ml | 2.73 ml | 5.459 ml |
10 mM | 0.273 ml | 1.365 ml | 2.73 ml |
5 mM | 0.055 ml | 0.273 ml | 0.546 ml |
biological activity | HT-2157(SNAP) is a selective high-affinity galanin -3 receptor (Gal3) competitive antagonists. |
Target | Galanin-3 receptor |