AMN082 dihydrochloride
Names
[ CAS No. ]:
97075-46-2
[ Name ]:
AMN082 dihydrochloride
[Synonym ]:
5-OMe-UDP trisodium salt
AMN 082 dihydrochloride
Biological Activity
[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]:
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C28H30Cl2N2
[ Molecular Weight ]:
465.45700
[ Exact Mass ]:
464.17900
[ PSA ]:
24.06000
[ LogP ]:
8.13060
Safety Information
[ Hazard Codes ]:
Xi