SR 48692 Property

Density 

1.50

storage temp. 

-20°C

solubility 

DMSO: ≥2mg/mL (warmed)

form 

powder

color 

white to beige

Safety

WGK Germany 

3

RTECS 

YD1988500

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

SR 48692 Chemical Properties,Usage,Production

Uses

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

Definition

ChEBI: 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-3-pyrazolyl]-oxomethyl]amino]-2-adamantanecarboxylic acid is a N-acyl-amino acid.

Biological Activity

ki: 8.6 nm for ht-29 cellssr 48692 is a nonpeptide neurotensin antagonist.neurotensin is a tridecapeptide and is distributed in both the central and peripheral nervous systems. neurotensin shows a wide spectrum of biological activities resulting in fulfilling a dual function as a neurotransmitter/neuromodulator in the brain and working as a hormone/cellular mediator in peripheral tissues.

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.

in vitro

sr 48692 was found to inhibit the binding of [3h]- or [125i]-neurotensin to membrane preparations from mouse brains and ht-29 cells. in ht-29 cells, sr 48692 also antagonized the neurotensin-induced mobilization of intracellular calcium, which was consistent with previous findings. moreover, in rat cerebellar slices, sr 48692 could block the cyclic gmp level increase in a dose-dependent manner [1].

in vivo

sr 48692 could antagonize the increase in rat brain mesolimbic dopamine turnover which was induced by the systemically active neurotensin peptide ei. whereas, sr 48692 did not antagonize ei-induced decrease in mouse body temperature and spontaneous locomotor activity [1].

storage

Store at +4°C

References

[1] pugsley ta,akunne hc,whetzel sz,demattos s,corbin ae,wiley jn,wustrow dj,wise ld,heffner tg. differential effects of the nonpeptide neurotensin antagonist, sr 48692, on the pharmacological effects of neurotensin agonists. peptides.1995;16(1):37-44.
[2] zerbib f,piche t,charles f,galmiche jp,bruley des varannes s. sr 48692, a specific neurotensin receptor antagonist, has no effect on oesophageal motility in humans. aliment pharmacol ther.2004 apr 15;19(8):931-9.