Neuroprotective effects of (+/-)-huprine Y on in vitro and in vivo models of excitoxicity damage

Exp Neurol. 2003 Apr;180(2):123-30. doi: 10.1016/s0014-4886(02)00029-8.

Abstract

We have investigated the neuroprotective effects of (+/-)-huprine Y on excitotoxic lesions in rat cerebellar granule cells (CGCs). (+/-)-Huprine Y prevented cell death induced by 100 microM glutamate, as well as, 10 microM MK-801, a NMDA receptor antagonist, in a significant manner. On the other hand, intracellular calcium increase induced by NMDA (200 microM), measured by fura-2 fluorescence, was prevented by (+/-)-huprine Y with an EC(50) of 12.44 microM, which evidences the modulatory action of this compound on NMDA-induced calcium currents. In vivo, we have studied (+/-)-huprine Y neuroprotective effects on striatal lesions induced by the subacute administration of the mitochondrial toxin 3-nitropropionic acid (3-NP, 30 mg/kg, ip, for 10 days). We have assessed that both the behavioral and the morphological consequences of the lesion were prevented by pretreatment with (+/-)-huprine Y (2.5 mg/kg/twice a day, ip). Striatal gliosis induced by 3-NP treatment was prevented by (+/-)-huprine Y pretreatment, as demonstrated by the attenuation of both the increase in [(3)H]PK 11195 specific binding indicative of microgliosis and the expression of hsp27 kDa, a chaperone expressed mainly in astrocytes. In conclusion, (+/-)-huprine Y attenuated excitotoxic-induced lesions, both in vitro and in vivo, and further evidence is provided for the potential use of this compound in the prevention of neurodegenerative disorders.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / pharmacology*
  • Animals
  • Binding, Competitive / drug effects
  • Calcium / metabolism
  • Cell Death / drug effects
  • Cells, Cultured
  • Cerebellum / cytology
  • Corpus Striatum / drug effects
  • Corpus Striatum / pathology
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Female
  • Gliosis / chemically induced
  • Gliosis / prevention & control
  • Glutamic Acid / toxicity
  • HSP27 Heat-Shock Proteins
  • Heat-Shock Proteins*
  • Heterocyclic Compounds, 4 or More Rings / pharmacology*
  • Isoquinolines / pharmacokinetics
  • Mice
  • Molecular Chaperones
  • Motor Activity / drug effects
  • N-Methylaspartate / pharmacology
  • Neoplasm Proteins / biosynthesis
  • Neurodegenerative Diseases / chemically induced
  • Neurodegenerative Diseases / pathology
  • Neurodegenerative Diseases / prevention & control*
  • Neurons / cytology
  • Neurons / drug effects*
  • Neuroprotective Agents / pharmacology*
  • Neurotoxins / toxicity*
  • Nitro Compounds
  • Propionates
  • Rats

Substances

  • Aminoquinolines
  • HSP27 Heat-Shock Proteins
  • Heat-Shock Proteins
  • Heterocyclic Compounds, 4 or More Rings
  • Hsbp1 protein, mouse
  • Hspb1 protein, rat
  • Isoquinolines
  • Molecular Chaperones
  • Neoplasm Proteins
  • Neuroprotective Agents
  • Neurotoxins
  • Nitro Compounds
  • Propionates
  • huprine Y
  • Glutamic Acid
  • N-Methylaspartate
  • 3-nitropropionic acid
  • Calcium
  • PK 11195