83027-13-8

83027-13-8 structure

Name: AMN082 free base
Chemical Name: AMN 082 dihydrochloride,N,N'-Bis(diphenylmethyl)-1,2-ethanediaminedihydrochloride
CAS Number: 83027-13-8
Molecular Formula: C₂₈H₂₈N₂
Molecular Weight: 465.45700
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2018-12-26 16:10:26
Modify Date: 2024-01-13 12:45:36
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects[1][2].

Name	AMN 082 dihydrochloride,N,N'-Bis(diphenylmethyl)-1,2-ethanediaminedihydrochloride
Synonyms	N,N'-diazenediyl-bis-phthalimide 1,4-bis-phthaloyltetrazene N,N'-Dibenzhydryl-aethylendiamin N,N'-dibenzhydryl-ethane-1,2-diamine 1,4-Bisphthalyl-tetrazen N,N'-dibenzhydryl-ethylenediamine Phthalimide,N,N'-azodi AMN 082

Description	AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	mGluR7[1]
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].
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].
References	[1]. Mitsukawa K, et al. A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo. Proc Natl Acad Sci U S A. 2005;102(51):18712-18717. [2]. Wang CC, et al. Metabotropic glutamate 7 receptor agonist AMN082 inhibits glutamate release in rat cerebral cortex nerve terminal. Eur J Pharmacol. 2018;823:11-18. [3]. Jenda M, et al. AMN082, a metabotropic glutamate receptor 7 allosteric agonist, attenuates locomotor sensitization and cross-sensitization induced by cocaine and morphine in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2015;57:166-175.

Boiling Point	533.7ºC at 760 mmHg
Molecular Formula	C₂₈H₂₈N₂
Molecular Weight	465.45700
Flash Point	321.5ºC
Exact Mass	464.17900
PSA	24.06000
LogP	8.13060

HS Code	2921590090

64042-50-8

~40%

119-61-9

83027-13-8

Literature: Koch, Russell W.; Dessy, Raymond E. Journal of Organic Chemistry, 1982 , vol. 47, # 23 p. 4452 - 4459

Precursor 1
64042-50-8
DownStream 0

HS Code	2921590090
Summary	2921590090. other aromatic polyamines and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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