1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. AMN082

AMN082 

Cat. No.: HY-103565
Handling Instructions

AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.

For research use only. We do not sell to patients.

AMN082 Chemical Structure

AMN082 Chemical Structure

CAS No. : 97075-46-2

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Description

AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects[1][2].

In Vitro

Preincubation of the synaptosomes with AMN082 (1 μM) for 10 min before 4-aminopyridine treatment efficiently inhibits the 4-aminopyridine-evoked release of glutamate, without altering the basal release of glutamate[2].

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

In Vivo

AMN082 (6 mg/kg; p.o.) induces stress hormone increases in an mGluR7-dependent fashion in mGluR7+/+ mice (C57BL/6 genetic background)[1].
AMN082 (1.25-5.0 mg/kg, i.p.; 30 min before every Cocaine or Morphine injection during repeated drug administration or before Cocaine or Morphine challenge) dose-dependently attenuates the development, as well as the expression of Cocaine or Morphine locomotor sensitization[3].

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

Animal Model: Male Swiss mice (20-25g)[3]
Dosage: 1.25, 2.5, 5.0 mg/kg
Administration: I.p.; given 30 min prior to Cocaine (10 mg/kg) or Morphine (10 mg/kg) challenge on day 17 or 20, respectively
Result: Significantly attenuated the expression of Cocaine-induced locomotor sensitization; Attenuated the induction of Morphine-induced sensitization.
Molecular Weight

465.46

Formula

C₂₈H₃₀Cl₂N₂

CAS No.

97075-46-2

SMILES

[H]Cl.[H]Cl.C(NCCNC(C1=CC=CC=C1)C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AMN082AMN 082AMN-082mGluRMetabotropic glutamate receptorsallostericoralblood-brainbarrierlocomotorsensitizationstresshormoneInhibitorinhibitorinhibit

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AMN082
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