化合物HT-2157;化合物HT-2157,10 MM DMSO 溶液;1-苯基-3-((3-(三氟甲基)苯基)亚氨基)二氢吲哚-2-酮;HT-2157试剂;HT-2157 ,S0014;HT-2157试剂; 1-phenyl-3-[[3-(trifluoromethyl)-phenol]-imino]-1H-indol-2-one; 1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-1H-indol-2-one
用途
- 生物活性
HT-2157(SNAP 37889) 是一种选择性的高亲和力甘丙肽-3 受体 (Gal3) 竞争性拮抗剂。
- 靶点
Galanin-3 receptor
- 体外研究
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.
- 体内研究
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.
