| Cas No.: | 146362-70-1 |
| Chemical Name: | Tricyclo[3.3.1.13,7]decane-2-carboxylicacid,2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]- |
| Synonyms: | Tricyclo[3.3.1.13,7]decane-2-carboxylicacid,2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-;2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid;SR 48692;Tricyclo[3.3.1.13,7]decane-2-carboxylicacid,2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphe...;2-({[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)tricyclo[3.3.1.1~3,7~]decane-2-carboxylic acid;Meclinertant;Reminertant;SR-48692;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;2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]tricyclo[3.3.1.1(3,7)]decane-2-carboxylic acid;2-CARBOXYLIC ACID;meclinertant, CID 119192;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 |
| SMILES: | COC1=C(C(OC)=CC=C1)C2N(N=C(C=2)C(=O)NC3(C(O)=O)C4CC5CC3CC(C5)C4)C6C7C(=CC(Cl)=CC=7)N=CC=6 |
| Formula: | C32H31N4O5Cl |
| M.Wt: | 587.06534 |
| Purity: | 99% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects[1][2][3]. |
| Target: | Neurotensin receptor 1 (NTS1)[1] |
| In Vivo: | Meclinertant (SR 48692) treatment reverses at 80 μg/kg the turning behavior induced by intrastriatal injection of neurotensin in mice and with a long duration of action (6 hours)[1]. |
| In Vitro: | In vitro, Meclinertant (SR 48692) competitively inhibits 125I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC50 values of 0.99 nM (guinea pig), 4.0 nM (rat mesencephalic cells), 7.6 nM (COS-7 cells transfected with the cloned high-affinity rat brain receptor), 13.7 nM (newborn mouse brain), 17.8 nM (newborn human brain), 8.7 nM (adult human brain), and 30.3 nM (HT-29 cells). Meclinertant also displaces 125I-labeled neurotensin from the low-affinity levocabastine-sensitive binding sites but at higher concentrations (34.8 nM for adult mouse brain and 82.0 nM for adult rat brain)[1]. In guinea pig striatal slices, Meclinertant blocks K+-evoked release of [3H]dopamine stimulated by neurotensin with a potency (IC50 = 0.46 nM) that correlates with its binding affinity[1]. |
| References: | [1]. Gully D, et al. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9. [2]. Griebel G, et al. Characterization of the profile of neurokinin-2 and neurotensin receptor antagonists in the mouse defense test battery. Neurosci Biobehav Rev. 2001 Dec;25(7-8):619-26. [3]. Felszeghy K, et al. Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference. Neuropsychopharmacology. 2007 Dec;32(12):2601-10. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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| 2018-0101 |
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