2. GPCR/G Protein Neuronal Signaling
  3. Neurotensin Receptor
  4. SR 142948

SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (SR 142948 dihydrochloride) usually boasts enhanced water solubility and stability.

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SR 142948 Chemical Structure

SR 142948 Chemical Structure

CAS No. : 184162-64-9

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Description

SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].

In Vitro

SR 142948 (1 µM; 90 min) inhibits expression of c-fos and krox24 in CHO-hNT1-R cells[1].
SR 142948 (0-1 µM; 1 h) exhibits good antagonistic activity by inhibiting [125I-Tyr3]NT binds to h-NTR1-CHO and HT 29 cell membranes, with IC50s of 1.19 and 0.32 nM, respectively[2].
SR 142948 (0-1 µM; 30 min) antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner[2].
SR 142948 (1, 10 nM; 60-80 s) antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SR 142948 Related Antibodies
In Vivo

SR 142948 (2 µg/kg; p.o.; single) inhibits the turning behavior induced by NT (10 pg/mouse)[2].
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner[2].
SR 142948 (0-10 mg/kg; p.o.; single) partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Swiss albino CD1 mice (25-30 g; intrastriatal injection of 10 pg/mouse NT)[2].
Dosage: 2 µg/kg
Administration: Oral administration; single.
Result: Inhibited the turning behavior with maximal and significant antagonism between 1-2 h after administration.
Molecular Weight

685.85

Formula

C39H51N5O6
CAS No.
SMILES

O=C(C1=NN(C2=C(C=C(C(N(C)CCCN(C)C)=O)C=C2)C(C)C)C(C3=C(C=CC=C3OC)OC)=C1)NC4([C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)C(O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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SR 142948 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SR 142948184162-64-9SR142948SR-142948Neurotensin Receptordopaminepsychotic disordersneurotensinHT 29CHO cellsInhibitorinhibitorinhibit

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