SR 48692
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
- CAS NO.:146362-70-1
- Empirical Formula: C32H31ClN4O5
- Molecular Weight: 587.07
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-05 21:24:55
What is SR 48692?
The Uses of SR 48692
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
What are the applications of Application
SR 48692 is a neurotensin inhibitor
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.
Properties of SR 48692
Density | 1.50 |
storage temp. | -20°C |
solubility | DMSO: ≥2mg/mL (warmed) |
form | powder |
color | white to beige |
Safety information for SR 48692
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for SR 48692
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