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SML0278

Sigma-Aldrich

SR 48692

≥98% (HPLC)

Sinónimos:

2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid, Meclinertant

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About This Item

Fórmula empírica (notación de Hill):
C32H31ClN4O5
Número de CAS:
146362-70-1
Peso molecular:
587.07
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
329825286
NACRES:
NA.77

Ensayo

≥98% (HPLC)

Formulario

powder

color

white to beige

solubilidad

DMSO: ≥2 mg/mL (warmed)

temp. de almacenamiento

−20°C

cadena SMILES

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)

Clave InChI

DYLJVOXRWLXDIG-UHFFFAOYSA-N

Información sobre el gen

human ... NTSR1(4923)

Aplicación

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

Acciones bioquímicas o fisiológicas

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.
SR 48692 is a high affinity, orally bioavailable and selective nonpeptide NT1 neurotensin receptor antagonist.

Características y beneficios

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.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
0000409727
0000409727
0000334724
0000337642
0000205595

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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
Polina Petkova-Kirova et al.
Brain research bulletin, 77(2-3), 129-135 (2008-08-30)
The effects of the peptide transmitter neurotensin (NT) on the release of acetylcholine (ACh), gamma-aminobutyric acid (GABA), glutamate (Glu), aspartate (Asp), and taurine from the prefrontal cortex (PFC) of freely moving rats were studied by transversal microdialysis. Neurotensin (0.2 and
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
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
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.
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