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

SR 142948 dihydrochloride 

Cat. No.: HY-107664A
Handling Instructions

SR 142948 dihydrochloride 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 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders.

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SR 142948 dihydrochloride Chemical Structure

SR 142948 dihydrochloride Chemical Structure

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Description

SR 142948 dihydrochloride 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 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].

In Vitro

SR 142948 (1 µM; 90 min) dihydrochloride inhibits expression of c-fos and krox24 in CHO-hNT1-R cells[1].
SR 142948 (0-1 µM; 1 h) dihydrochloride 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) dihydrochloride 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) dihydrochloride antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

SR 142948 (2 µg/kg; p.o.; single) dihydrochloride inhibits the turning behavior induced by NT (10 pg/mouse)[2].
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) dihydrochloride 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) dihydrochloride partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)[2].

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

758.77

Appearance

Solid

Formula

C39H53Cl2N5O6
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([[email protected]]5C[[email protected]](C6)C[[email protected]@H]4C[[email protected]]6C5)C(O)=O.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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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.

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Keywords:

SR 142948SR142948SR-142948Neurotensin ReceptorOrallyneurotensin receptorNTh-NTR1-CHOHT-29inositol monophosphatehypothermiaanalgesiasteeringblood-brain permeabilitypsychiatric disordersInhibitorinhibitorinhibit

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