质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: ≥2 mg/mL (warmed)
储存温度
−20°C
SMILES字符串
COc1cccc(OC)c1-c2cc(nn2-c3ccnc4cc(Cl)ccc34)C(=O)NC5(C6CC7CC(C6)CC5C7)C(O)=O
InChI
1S/C32H31ClN4O5/c1-41-27-4-3-5-28(42-2)29(27)26-16-24(36-37(26)25-8-9-34-23-15-21(33)6-7-22(23)25)30(38)35-32(31(39)40)19-11-17-10-18(13-19)14-20(32)12-17/h3-9,15-20H,10-14H2,1-2H3,(H,35,38)(H,39,40)
InChI key
DYLJVOXRWLXDIG-UHFFFAOYSA-N
基因信息
human ... NTSR1(4923)
应用
SR 48692 has been used as a neurotensin high-affinity receptor 1 (NTSR1) antagonist:
- to explore the function of NTSR1 in glioblastoma (GBM) cells
- to determine the roles of neurotensin (NT) in the regulation of bile acid (BA) uptake, in vivo
- to explore the involvement of NTSR1 versus NTSR2 in mice
生化/生理作用
SR 48692 is a high affinity, orally bioavailable and selective nonpeptide NT1 neurotensin receptor antagonist that antagonizes neurotensin-induced calcium mobilization with a pA2 of 8.13 in HT-29 human colon carcinoma cell line, and blocks the ability of neurotensin to increase GABA levels in the prefrontal cortex.
特点和优势
This compound is featured on the Neurotensin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Kristóf László et al.
Behavioural brain research, 208(2), 430-435 (2009-12-29)
In the central nervous system neurotensin (NT) acts as a neurotransmitter and neuromodulator. It was shown that NT has positive reinforcing effects after its direct microinjection into the ventral tegmental area. The central nucleus of amygdala (CeA), part of the
C Jomphe et al.
The European journal of neuroscience, 24(10), 2789-2800 (2006-11-23)
Several lines of evidence suggest a close association between dopamine (DA) and neurotensin (NT) systems in the CNS. Indeed, in the rodent brain, abundant NT-containing fibres are found in DA-rich areas such as the ventral tegmental area and substantia nigra.
Kristóf László et al.
Behavioural brain research, 226(2), 597-600 (2011-09-29)
Tridecapeptide neurotensin (NT) acts as a neurotransmitter and/or neuromodulator and plays a role in learning and reinforcement. The central nucleus of amygdala (CeA), which is relatively rich in NT and neurotensin-1 receptors (NTS1), participates in the regulation of memory and
James B Thomas et al.
Bioorganic & medicinal chemistry letters, 19(5), 1438-1441 (2009-02-07)
In a search for nonpeptide agonists for the neurotensin receptor (NTR1), we replaced the adamantyl amino acid moiety found in the antagonist SR48692 (1a) with leucine and related alpha-alkylamino acids found in peptide agonists. When tested in a calcium mobilization
Fabiana G Costa et al.
Neuropeptides, 41(2), 83-91 (2007-02-06)
Psychostimulant-induced locomotor sensitization has been related to changes within the mesolimbic dopamine system and has been suggested to be useful to study mechanisms underlying drug craving. Neurotensin is a neuropeptide co-localized with dopamine in the mesolimbic system. The response to
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