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SML0278

SR 48692

Name: SR 48692
Brand: SIGMA

≥98% (HPLC), nonpeptide NT1 neurotensin receptor antagonist , powder

Synonym(s):

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

Empirical Formula (Hill Notation):

C₃₂H₃₁ClN₄O₅

CAS Number:

146362-70-1

Molecular Weight:

587.07

UNSPSC Code:

12352200

PubChem Substance ID:

329825286

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Properties

Product Name

SR 48692, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥2 mg/mL (warmed)

storage temp.

−20°C

SMILES string

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

Gene Information

human ... NTSR1(4923)

Description

Application

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

Biochem/physiol Actions

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.

Features and Benefits

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Bidirectional regulation of dopamine D2 and neurotensin NTS1 receptors in dopamine neurons.

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.

The role of neurotensin in positive reinforcement in the rat central nucleus of amygdala.

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

The role of neurotensin in passive avoidance learning in the rat central nucleus of amygdala.