SNAP-37889

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性甘丙肽 3 受体 (Gal3) 拮抗剂，Ki 为 17.44 nM，对 Gal3 的选择性高于 Gal1 和 Gal2 亚型（Ki 均 >10 uM）。

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.

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.

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.

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

GPCR/G Protein

Galanin Receptor

Galanin Receptor

Neurological Disease

Depression

303149-14-6

366.3359

C21H13F3N2O

>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

2H-Indol-2-one, 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-

(-20℃)

With Ice Pack

≥ 2 years