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| | SR 48692 Basic information |
| Product Name: | SR 48692 | | Synonyms: | SR 48692;2-CARBOXYLIC ACID;2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid;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, CID 119192;Meclinertant;merclinertant;CS-334 | | CAS: | 146362-70-1 | | MF: | C32H31ClN4O5 | | MW: | 587.07 | | EINECS: | | | Product Categories: | | | Mol File: | 146362-70-1.mol |  |
| | SR 48692 Chemical Properties |
| density | 1.50 | | storage temp. | -20°C | | solubility | DMSO: ≥2mg/mL (warmed) | | form | powder | | color | white to beige |
| WGK Germany | 3 | | RTECS | YD1988500 |
| | SR 48692 Usage And Synthesis |
| 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. |
| | SR 48692 Preparation Products And Raw materials |
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