The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel alpha7 ligand, is prevented through angiotensin II activation of a tyrosine phosphatase

J Pharmacol Exp Ther. 2004 Apr;309(1):16-27. doi: 10.1124/jpet.103.061655. Epub 2004 Jan 13.

Abstract

We have recently provided evidence for nicotine-induced complex formation between the alpha7 nicotinic acetylcholine receptor (nAChR) and the tyrosine-phosphorylated enzyme Janus kinase 2 (JAK2) that results in subsequent activation of phosphatidylinositol-3-kinase (PI-3-K) and Akt. Nicotine interaction with the alpha7 nAChR inhibits Abeta (1-42) interaction with the same receptor, and the Abeta (1-42)-induced apoptosis is prevented through nicotine-induced activation of JAK2. These effects can be shown by measuring markers of cytotoxicity, including the cleavage of the nuclear protein poly(ADP-ribose) polymerase (PARP), the induction of caspase 3, or cell viability. In this study, we found that 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel alpha7-selective agonist, exerts neuroprotective effects via activation of the JAK2/PI-3K cascade, which can be neutralized through activation of the angiotensin II (Ang II) AT(2) receptor. Vanadate not only augmented the TC-1698-induced tyrosine phosphorylation of JAK2 but also blocked the Ang II neutralization of TC-1698-induced neuroprotection against Abeta (1-42)-induced cleavage of PARP. Furthermore, when SHP-1 was neutralized via antisense transfection, the Ang II inhibition of TC-1698-induced neuroprotection against Abeta (1-42) was prevented. These results support the main hypothesis that states that JAK2 plays a central role in the nicotinic alpha7 receptor-induced activation of the JAK2-PI-3K cascade in PC12 cells, which ultimately contribute to nAChR-mediated neuroprotection. Ang II inhibits this pathway through the AT(2) receptor activation of the protein tyrosine phosphatase SHP-1. This study supports central and opposite roles for JAK2 and SHP-1 in the control of apoptosis and alpha7-mediated neuroprotection in PC12 cells.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Angiotensin II / metabolism*
  • Animals
  • Apoptosis
  • Bridged Bicyclo Compounds / pharmacology*
  • Drosophila Proteins
  • Enzyme Activation
  • Intracellular Signaling Peptides and Proteins
  • Janus Kinase 2
  • Neuroprotective Agents / pharmacology*
  • PC12 Cells
  • Phosphatidylinositol 3-Kinases / metabolism
  • Phosphorylation
  • Protein Serine-Threonine Kinases*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 6
  • Protein Tyrosine Phosphatases / metabolism*
  • Protein-Tyrosine Kinases / metabolism*
  • Proto-Oncogene Proteins / metabolism
  • Proto-Oncogene Proteins c-akt
  • Pyridines / pharmacology*
  • Rats
  • Receptors, Nicotinic / metabolism*
  • Serine / metabolism
  • Tyrosine / metabolism
  • Tyrphostins / pharmacology
  • alpha7 Nicotinic Acetylcholine Receptor

Substances

  • 2-(3-pyridyl)-1-azabicyclo(3.2.2)nonane
  • Bridged Bicyclo Compounds
  • Chrna7 protein, rat
  • Drosophila Proteins
  • Intracellular Signaling Peptides and Proteins
  • Neuroprotective Agents
  • Proto-Oncogene Proteins
  • Pyridines
  • Receptors, Nicotinic
  • Tyrphostins
  • alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide
  • alpha7 Nicotinic Acetylcholine Receptor
  • nicotinic acetylcholine receptor alpha-subunits, Drosophila
  • Angiotensin II
  • Tyrosine
  • Serine
  • Protein-Tyrosine Kinases
  • Jak2 protein, rat
  • Janus Kinase 2
  • Akt1 protein, rat
  • Protein Serine-Threonine Kinases
  • Proto-Oncogene Proteins c-akt
  • Protein Tyrosine Phosphatase, Non-Receptor Type 6
  • Protein Tyrosine Phosphatases
  • Ptpn6 protein, rat