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HT-2157
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HT-2157图片
CAS NO:303149-14-6
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 366.34
Formula C21H13F3N2O
CAS No. 303149-14-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 29 mg/mL
Water: < 1 mg/mL
Ethanol: < 1 mg/mL
SMILES O=C1N(C2=CC=CC=C2)C3=C(C=CC=C3)/C1=N/C4=CC=CC(C(F)(F)F)=C4
Synonyms HT-2157; HT2157; HT 2157; SNAP37889; SNAP 37889; SNAP-37889;
实验参考方法
In Vitro

In vitro activity: HT-2157 (also known as SNAP 37889) is a selective, high-affinity, and competitive antagonists of galanin-3 receptor (Gal3) that has the potential for the treatment of major depressive disorder. Acute administration of SNAP 37889 or the more soluble analog SNAP 398299 enhanced rat social interaction. Furthermore, acute SNAP 37889 was also shown to reduce guinea pig vocalizations after maternal separation, to attenuate stress-induced hyperthermia in mice, to increase punished drinking in rats, and to decrease immobility and increase swimming time during forced swim tests with rats. Moreover, SNAP 37889 increased the social interaction time after 14 days of treatment and maintained its antidepressant effects during forced swim tests with rats after 21 days of treatment. In microdialysis studies, SNAP 37889 partially antagonized the galanin-evoked reduction in hippocampal serotonin (5-hydroxytryptamine, 5-HT), as did the 5-HT(1A) receptor antagonist WAY100635.


Kinase Assay: Binding affinities for HT-2157 (SNAP 37889) and SNAP 398299 at the human Gal1, Gal2, and Gal3 receptors are determined by using the 125I-galanin displacement assay. Additionally, is tested for binding in a broad cross-reactivity panel that included G-protein-coupled receptors, ion channels, enzymes, and transporters. The ability of HT-2157 to antagonize functional responses to galanin is examined in modified HEK-293 cells (PEAKrapid cells) transiently cotransfected with the Gal3 receptor and Gαz by measuring the inhibition of adenylyl cyclase activity.


Cell Assay: 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 VivoThe 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.
Animal modelRats
Formulation & Dosage30 mg/kg, i.p
References Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94; Regul Pept. 2011 Jan 17;166(1-3):59-67.