An allosteric antagonist of NTS1 (Kd = 3.4 nM); inhibits neurotensin binding to brain tissue from guinea pig

SR 48692 – 10 mg

Brand:
Cayman
CAS:
146362-70-1
Storage:
-20
UN-No:
Non-Hazardous - /

SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).{35296,35297} SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells with IC50 values ranging from 0.99 to 30.3 nM.{35296} It blocks neurotensin-induced intracellular calcium mobilization in HT-29 cells with a Ki value of 7.4 nM. SR 48692 (10 μM) inhibits NCI-H209 and NCI-H345 cell proliferation by approximately 70 and 80%, respectively.{35299} In vivo, SR 48692 (10 μg per day) reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model. SR 48692 (80 μg/kg, p.o.) reduces contralateral turning induced by neurotensin (Item No. 24717) administration in mice by 85%.{35296} Daily administration of SR 48692 for five days in rats delays sensitization to the locomotor activating effects of cocaine during three additional cocaine challenges when given seven days prior to cocaine delivery but not under a cotreatment regimen.{35298}  

 

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Description

An allosteric antagonist of NTS1 (Kd = 3.4 nM); inhibits neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells (IC50s = 0.99-30.3 nM); blocks neurotensin induced intracellular calcium mobilization in HT-29 cells (Ki = 7.4 nM); reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model (10 μg per day); reduces contralateral turning induced by neurotensin administration in mice by 85% (80 μg/kg, p.o.); delays sensitization to the locomotor activating effects of cocaine in rats when administered prior to cocaine delivery and not concomitantly

Formal name: 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid

Synonyms: 

Molecular weight: 587.1

CAS: 146362-70-1

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Cancer||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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