Spiro[imidazo[1,2-a]pyridine-3,2-indan]-2(3H)-one (ZSET1446/ST101) treatment rescues olfactory bulbectomy-induced memory impairment by activating Ca2+/calmodulin kinase II and protein kinase C in mouse hippocampus

J Pharmacol Exp Ther. 2008 Jul;326(1):127-34. doi: 10.1124/jpet.108.137471. Epub 2008 Apr 3.

Abstract

Olfactory bulbectomy (OBX) in mice elicits impaired memory and cognitive functions. Here, we found that chronic oral administration of spiro[imidazo[1,2-a]pyridine-3,2-indan]-2(3H)-one (ZSET1446/ST101) (0.1-1 mg/kg/day), a novel cognitive enhancer, significantly improved memory deficits as assessed by Y-maze and novel object recognition tasks in OBX mice. Immunostaining of cholinergic neurons in the medial septum by using an anti-choline acetyltransferase antibody indicated that chronic ZSET1446 treatment did not rescue cholinergic neurons. However, chronic treatment significantly restored OBX-induced decreases both in calcium/calmodulin-dependent protein kinase II (CaMKII) and protein kinase C (PKC) phosphorylation without improving decreased extracellular signal-regulated kinase phosphorylation in the hippocampal CA1 region. Consistent with enhanced CaMKII and PKC phosphorylation, ZSET1446 treatment improved glutamate receptor 1 (Ser-831) phosphorylation in the hippocampal CA1 region. ZSET1446 treatment also significantly rescued impaired long-term potentiation (LTP) in the hippocampal CA1 region of OBX mice. Taken together, the cognition-enhancing effect of ZSET1446 is probably mediated in part by stimulation of CaMKII and PKC activities, which in turn rescue impaired hippocampal LTP in OBX mice.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium-Calmodulin-Dependent Protein Kinase Type 2 / metabolism*
  • Enzyme Activation / drug effects
  • Enzyme Activation / physiology
  • Hippocampus / drug effects
  • Hippocampus / enzymology*
  • Indans / pharmacology
  • Indans / therapeutic use*
  • Male
  • Memory Disorders / drug therapy
  • Memory Disorders / enzymology*
  • Mice
  • Olfactory Bulb / enzymology*
  • Olfactory Bulb / surgery
  • Protein Kinase C / metabolism*
  • Spiro Compounds / pharmacology
  • Spiro Compounds / therapeutic use*
  • Treatment Outcome

Substances

  • Indans
  • Spiro Compounds
  • spiro(imidazo-(1,2-a)pyridine-3,2-indan)-2(3H)-one
  • Protein Kinase C
  • Calcium-Calmodulin-Dependent Protein Kinase Type 2