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About This Item
Empirical Formula (Hill Notation):
C28H28N2 · 2HCl
CAS Number:
Molecular Weight:
465.46
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
assay
≥98% (HPLC)
form
solid
storage condition
desiccated
color
white to off-white
solubility
DMSO: ≥5 mg/mL
storage temp.
−20°C
SMILES string
Cl[H].Cl[H].C(CNC(c1ccccc1)c2ccccc2)NC(c3ccccc3)c4ccccc4
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
InChI key
YRQCDCNQANSUPB-UHFFFAOYSA-N
Application
AMN082 is a selective allosteric mGluR 7 receptor agonist and has been used to study the role of this glutamate receptor type in the medial prefrontal cortex in mice. AMN082 inhibits forskolin-stimulated cAMP accumulation, and stimulates not only GTPγS binding but also the release of stress hormones.
Biochem/physiol Actions
AMN082 is a selective allosteric mGluR 7 receptor agonist and first selective pharmacological tool for mGluR7. AMN082 inhibits forskolin-stimulated cAMP accumulation (EC50 = 64 nM) and stimulates GTPγS binding (EC50 = 290 nM) similar to L-AP4 and greater than L-glutamate. Thus, AMN082 is a "full agonist" and acts at an allosteric site in the transmembrane domain of mGluR7. AMN082 has no effects at other mGluR′s up to 10 μM and stimulates release of stress hormones (corticosterone and ACTH) and is orally active and brain penetrable.
AMN082 is a selective allosteric mGluR 7 receptor agonist and first selective pharmacological tool for mGluR7. AMN082 stimulates the release of stress hormones (corticosterone and ACTH), orally active and brain penetrable.
Storage Class
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
Regulatory Information
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Articles
Sigma-Aldrich offers many products related to G-protein family glutamate receptors for your research needs.
Joanna M Wierońska et al.
Psychopharmacology, 220(3), 481-494 (2011-09-29)
Several studies have suggested that modulation of the glutamatergic system via metabotropic glutamate receptors (mGlu) could be a new and efficient way to achieve antipsychotic-like activity. Here, we decided to investigate the possible role of the group III mGlu receptor
Katharina Gryksa et al.
Genes, brain, and behavior, 19(1), e12627-e12627 (2019-12-04)
The group III metabotropic glutamate receptor subtype 7 (mGlu7) is an important regulator of glutamatergic and GABAergic neurotransmission and known to mediate emotionality and male social behavior. However, a possible regulatory role in maternal behavior remains unknown to date. Adequate
Tomoteru Yamasaki et al.
EJNMMI research, 3(1), 54-54 (2013-07-23)
Metabotropic glutamate 7 (mGlu7) receptor is a crucial target protein for the development of pharmaceuticals against central nervous system disorders. In the present study, we synthesized [11C]MMPIP, a putative radioligand for mGlu7 (binding constant KB = 30 nM), and evaluated