AMN082 dihydrochloride

Modify Date: 2024-01-05 08:45:36

AMN082 dihydrochloride structure	Common Name	AMN082 dihydrochloride
	CAS Number	97075-46-2	Molecular Weight	465.45700
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₈H₃₀Cl₂N₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of AMN082 dihydrochloride

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].

Name	N,N'-Bis(diphenylmethyl)-1,2-ethanediamine dihydrochloride
Synonym	More Synonyms

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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
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]. 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.
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.