An NTS1 agonist; selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM

ML314 – 25 mg

Brand:
Cayman
CAS:
1448895-09-7
Storage:
-20
UN-No:
Non-Hazardous - /

ML314 is a neurotensin-1 receptor (NTS1) agonist.{43308,43309} It is selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively) but is inactive in an NTS1 calcium flux assay (EC50 = >80 μM) indicating that, in contrast to other NTS1 agonists, it does not signal through the traditional Gq-coupled pathway.{43309} ML314 is also a positive allosteric modulator of NTS1 that increases binding of radiolabeled neurotensin (Item No. 24717) to NTS1 in a concentration-dependent manner.{43308} It reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice when administered at doses of 20 and 10 to 30 mg/kg, respectively.{43308} ML314 (30 mg/kg) also reduces methamphetamine self-administration in rats.  

 

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Description

An NTS1 agonist; selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively); inactive in an NTS1 calcium flux assay (EC50 = >80 μM); a positive allosteric modulator that increases binding of radiolabaled neurotensin to NTS1 in a concentration-dependent manner; reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice at 20 and 10-30 mg/kg, respectively; reduces methamphetamine self-administration in rats at 30 mg/kg,

Formal name: 2-cyclopropyl-6,7-dimethoxy-4-[4-(2-methoxyphenyl)-1-piperazinyl]-quinazoline

Synonyms: 

Molecular weight: 420.5

CAS: 1448895-09-7

Purity: ≥98%

Formulation: A crystalline solid

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

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