Structure
Meclinertant, Inhibitor
Meclinertant
Purity
98.00%
Synonyms
Meclinertant; SR 48692; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C32H31ClN4O5
SMILES
O=C(C1=NN(C2=CC=NC3=C2C=CC(Cl)=C3)C(C4=C(C=CC=C4OC)OC)=C1)NC5([C@H]6C[C@H](C7)C[C@@H]5C[C@H]7C6)C(O)=O
CAS Number
146362-70-1
Target & IC50
Neurotensin receptor 1 (NTS1)
In Vitro
Meclinertant displaces 125I-labeled neurotensin from the low-affinity levocabastine-sensitive binding sites but at higher concentrations (34.8nM for adult mouse brain and 82.0nM for adult rat brain). Meclinertant competitively inhibits 125I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC50 values of 0.99nM (guinea pig), 4.0nM (rat mesencephalic cells), 7.6nM (COS-7 cells transfected with the cloned high-affinity rat brain receptor), 13.7nM (newborn mouse brain), 17.8nM (newborn human brain), 8.7nM (adult human brain), and 30.3nM (HT-29 cells). Meclinertant blocks K+-evoked release of [3H]dopamine stimulated by neurotensin with a potency (IC50 = 0.46nM) that correlates with its binding affinity, in guinea pig striatal slices[1].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Meclinertant, inhibitor
Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cells. Meclinertant has anxiolytic, anti-addictive, and memory-impairing effects.
References
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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Product Notes
The Meclinertant (Catalog #AAA5755176) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Meclinertant, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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