Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 35 days | $ 78.00 | |
5 mg | 35 days | $ 297.00 | |
10 mg | 35 days | $ 575.00 |
Description | 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. |
In vitro | Meclinertant 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). Meclinertant competitively inhibits 125I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC50 values of 0.99 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 blocks K+-evoked release of [3H]dopamine stimulated by neurotensin with a potency (IC50 = 0.46 nM) that correlates with its binding affinity, in guinea pig striatal slices[1]. |
In vivo | Meclinertant (80 μg/kg; in mice) treatment, reverses the turning behavior caused by the intrastriatal injection of neurotensin. It also has a long duration of action (6 hours)[1]. |
Synonyms | SR 48692 |
Molecular Weight | 587.07 |
Formula | C32H31ClN4O5 |
CAS No. | 146362-70-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Meclinertant 146362-70-1 Others SR-48692 SR48692 SR 48692 inhibitor inhibit