A noncompetitive antagonist of mGluR1 (IC50 = 10.7 nM); selective over mGluR5 (IC50 = 343 nM)

A-841720 – 5 mg

Brand:
Cayman
CAS:
869802-58-4
Storage:
-20
UN-No:
Non-Hazardous - /

A-841720 is a noncompetitive antagonist of the group 1 metabotropic glutamate receptor mGluR1 with an IC50 value of 10.7 nM for inhibition of L-glutamate-induced calcium release in 1321 N1 cells.{40808} It is selective for mGluR1 over mGluR5 (IC50 = 343 nM) as well as mGluR2, mGluR4, and mGluR7, where it does not inhibit agonist-induced calcium release in HEK293 cells. It is also selective for mGluR1 over a panel of other G-coupled protein receptors as well as ligand- and voltage-gated ion channels at a concentration of 10 µM. A-841720 dose-dependently inhibits complete Freund’s adjuvant-induced inflammatory pain (ED50 = 23 µmol/kg) and sciatic nerve injury-induced mechanical allodynia (ED50 = 28 µmol/kg) in rats. It also enhances cocaine seeking in mice after a prolonged abstinence following a single conditioning session when administered at a dose of 10 mg/kg per day.{40809}  

 

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Description

A noncompetitive antagonist of mGluR1 (IC50 = 10.7 nM); selective over mGluR5 (IC50 = 343 nM), mGluR2, mGluR4, and mGluR7; selective over a panel of other G-coupled protein receptors as well as ligand- and voltage-gated ion channels at a concentration of 10 µM; dose-dependently inhibits complete Freund’s adjuvant-induced inflammatory pain (ED50 = 23 µmol/kg) and sciatic nerve injury-induced mechanical allodynia (ED50 = 28 µmol/kg) in rats; enhances cocaine seeking in mice after a prolonged abstinence following a single conditioning session (10 mg/kg)

Formal name: 9-(dimethylamino)-3-(hexahydro-1H-azepin-1-yl)-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one

Synonyms: 

Molecular weight: 343.5

CAS: 869802-58-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Pain Research

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