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

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.

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AMN082 Chemical Structure

AMN082 Chemical Structure

CAS No. : 97075-46-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 174 In-stock
Solution
10 mM * 1 mL in DMSO USD 174 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 170 In-stock
10 mg USD 280 In-stock
25 mg USD 580 In-stock
50 mg USD 930 In-stock
100 mg USD 1480 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

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

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
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (71.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1484 mL 10.7421 mL 21.4841 mL
5 mM 0.4297 mL 2.1484 mL 4.2968 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1484 mL 10.7421 mL 21.4841 mL 53.7103 mL
5 mM 0.4297 mL 2.1484 mL 4.2968 mL 10.7421 mL
10 mM 0.2148 mL 1.0742 mL 2.1484 mL 5.3710 mL
15 mM 0.1432 mL 0.7161 mL 1.4323 mL 3.5807 mL
20 mM 0.1074 mL 0.5371 mL 1.0742 mL 2.6855 mL
25 mM 0.0859 mL 0.4297 mL 0.8594 mL 2.1484 mL
30 mM 0.0716 mL 0.3581 mL 0.7161 mL 1.7903 mL
40 mM 0.0537 mL 0.2686 mL 0.5371 mL 1.3428 mL
50 mM 0.0430 mL 0.2148 mL 0.4297 mL 1.0742 mL
60 mM 0.0358 mL 0.1790 mL 0.3581 mL 0.8952 mL
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AMN082 Related Classifications

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  • 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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AMN082
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HY-103565
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