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HT-2157

CAS No. : 303149-14-6

MCE 站：HT-2157

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Neuropeptide Y Receptor

In Vitro: HT-2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK^- cells expressing the human Gal₃ receptor (K_i=17.44±0.01 nM; n>100) and is highly selective for Gal₃ over the Gal₁ and Gal₂ 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: 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.

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