SR 142948

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Cat.No. 2309 - SR 142948 | C39H51N5O6 | CAS No. 184162-64-9
Description: Highly potent NT receptor antagonist
Chemical Name: 2-[[[5-(2,6-Dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid
Purity: ≥97% (HPLC)
Datasheet
Citations (3)

Biological Activity

Potent non-peptide neurotensin (NT) receptor antagonist that binds with high affinity (IC50 = 0.32 - 3.96 nM; Ki < 10 nM). Attenuates amphetamine-induced hyperactivity and is orally active in vivo.

Technical Data

M. Wt 685.86
Formula C39H51N5O6
Storage Store at +4°C
Purity ≥97% (HPLC)
CAS Number 184162-64-9
PubChem ID 5311451
InChI Key LWULHXVBLMWCHO-UHFFFAOYSA-N
Smiles COC1=CC=CC(OC)=C1C1=CC(=NN1C1=C(C=C(C=C1)C(=O)N(C)CCCN(C)C)C(C)C)C(=O)NC1(C2CC3CC(C2)CC1C3)C(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.44 75
water 17.15 25

Preparing Stock Solutions

The following data is based on the product molecular weight 685.86. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.46 mL 7.29 mL 14.58 mL
5 mM 0.29 mL 1.46 mL 2.92 mL
10 mM 0.15 mL 0.73 mL 1.46 mL
50 mM 0.03 mL 0.15 mL 0.29 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Gully et al (1997) Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J.Pharmacol.Exp.Ther. 280 802 PMID: 9023294

Quere et al (1998) X-ray structural characterization of SR 142948, a novel potent synthetic neurotensin receptor antagonist. Bioorg.Med.Chem.Lett. 8 653 PMID: 9871577

Marie-Claire et al (2008) Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice. Neuropharmacology 54 1107 PMID: 18410947


If you know of a relevant reference for SR 142948, please let us know.

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Keywords: potent NT receptor antagonists Receptors Neurotensin SR142948 Neurotensin Receptors

3 Citations for SR 142948

Citations are publications that use Tocris products. Selected citations for SR 142948 include:

Yin et al (2008) Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling. Neuropharmacology 54 79 PMID: 17675102

Rouibi et al (2016) Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin. J Cereb Blood Flow Metab 9 470 PMID: 26733785

Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic Neurons. J Neurosci 35 11144 PMID: 26245975


Do you know of a great paper that uses SR 142948 from Tocris? If so please let us know.

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