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AMN 082 dihydrochloride

allosteric agonist of mGluR7 CAS# 97075-46-2

AMN 082 dihydrochloride

Catalog No. BCC7344----Order now to get a substantial discount!

Product Name & Size Price Stock
AMN 082 dihydrochloride: 5mg $69 In Stock
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Chemical structure

AMN 082 dihydrochloride

3D structure

Chemical Properties of AMN 082 dihydrochloride

Cas No. 97075-46-2 SDF Download SDF
PubChem ID 11698390 Appearance Powder
Formula C28H30Cl2N2 M.Wt 465.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 2 mM in water with gentle warming
Chemical Name N,N'-dibenzhydrylethane-1,2-diamine;dihydrochloride
SMILES C1=CC=C(C=C1)C(C2=CC=CC=C2)NCCNC(C3=CC=CC=C3)C4=CC=CC=C4.Cl.Cl
Standard InChIKey YRQCDCNQANSUPB-UHFFFAOYSA-N
Standard InChI InChI=1S/C28H28N2.2ClH/c1-5-13-23(14-6-1)27(24-15-7-2-8-16-24)29-21-22-30-28(25-17-9-3-10-18-25)26-19-11-4-12-20-26;;/h1-20,27-30H,21-22H2;2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AMN 082 dihydrochloride

DescriptionThe first selective mGlu7 agonist. Potently inhibits cAMP accumulation and stimulates GTPγS binding in recombinant cells and on membranes expressing mGlu7 (EC50 = 64 - 290 nM). Selective over other mGluR subtypes and selected ionotropic glutamate receptors up to 10 μM. Acts via a novel allosteric site and is orally active and brain penetrant. Reduces haloperidol-induced catalepsy in rats.

AMN 082 dihydrochloride Dilution Calculator

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Preparing Stock Solutions of AMN 082 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1485 mL 10.7423 mL 21.4846 mL 42.9692 mL 53.7115 mL
5 mM 0.4297 mL 2.1485 mL 4.2969 mL 8.5938 mL 10.7423 mL
10 mM 0.2148 mL 1.0742 mL 2.1485 mL 4.2969 mL 5.3711 mL
50 mM 0.043 mL 0.2148 mL 0.4297 mL 0.8594 mL 1.0742 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.4297 mL 0.5371 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AMN 082 dihydrochloride

AMN 082 dihydrochloride is an specific allosteric agonist of mGluR7 [1]. In the absence of orthosteric agonist, AMN 082 activated the human mGlu7 receptor with an EC50 of 64 nM in vitro [2].

MGlu receptors belong to the family 3 G-protein coupled receptors (GPCRs) [2]. The GPCR metabotropic glutamate receptor 7 (mGluR7) is widely expressed in the nervous system. MGluR7 is implicated in many physiological processes such as synaptic plasticity and neuroprotection [1].

Dissociated hippocampal cultured neurons had been transfected with N-terminally myc-tagged mGluR7a were used in the assay. In these neurons, treatment with AMN082 at concentrations ranging from 0.5-1 µM strikingly caused robust mGluR7 internalization. The receptor internalization was increased to 291 ± 30% of control levels. The binding site of AMN082 on mGluR7 is distinct from the glutamate binding pocket on the receptor, conventional competitive antagonists are not able to prevent the activation of the allosteric agonist to the receptor [1].

In vivo, treatment with AMN082 was shown to penetrate into the brain and hence it modulated the level of stress hormones (ACTH and cortisol) in wild type animal. But these effects were not found in the mGluR7 ko mouse [2].

References:
[1].  Pelkey KA, Yuan X, Lavezzari G, et al. mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082. Neuropharmacology, 2007, 52(1): 108-117.
[2].  Gasparini F, Spooren W. Allosteric modulators for mGlu receptors. Current neuropharmacology, 2007, 5(3): 187-194.

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References on AMN 082 dihydrochloride

Metabotropic glutamate 7 receptor subtype modulates motor symptoms in rodent models of Parkinson's disease.[Pubmed:19940105]

J Pharmacol Exp Ther. 2010 Mar;332(3):1064-71.

Metabotropic glutamate (mGlu) receptors modulate synaptic transmission in the central nervous system and represent promising therapeutic targets for symptomatic treatment of Parkinson's disease (PD). Among the eight mGlu receptor subtypes, mGlu7 receptor is prominently expressed in the basal ganglia, but its role in restoring motor function in animal models of PD is not known. The effects of N,N'-dibenzhydrylethane-1,2-diamine dihydrochloride (AMN082), the first selective allosteric activator of mGlu7 receptors, were thus tested in different rodent models of PD. Here, we show that oral (5 mg/kg) or intrastriatal administration (0.1 and 0.5 nmol) of AMN082 reverses haloperidol-induced catalepsy in rats. AMN082 (2.5 and 5 mg/kg) reduces apomorphine-induced rotations in unilateral 6-hydroxydopamine (6-OHDA)-lesioned rats. In a more complex task commonly used to evaluate major akinetic symptoms of PD patients, 5 mg/kg AMN082 reverses the increased reaction time to respond to a cue of bilateral 6-OHDA-lesioned rats. In addition, AMN082 reduces the duration of haloperidol-induced catalepsy in a mGlu7 receptor-dependent manner in wild-type but not mGlu7 receptor knockout mice. Higher doses of AMN082 (10 and 20 mg/kg p.o.) have no effect on the same models of PD. Overall these findings suggest that mGlu7 receptor activation can reverse motor dysfunction associated with reduced dopamine activity. Selective ligands of mGlu7 receptor subtypes may thus be considered as promising compounds for the development of antiparkinsonian therapeutic strategies.

Description

The first selective mGlu7 agonist

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