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Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of

Peter R Kufahl1, Natali E Nemirovsky1, Lucas R Watterson1

  • 1Department of Psychology, Arizona State University, Tempe, AZ, 85287-1104, USA.

F1000Research
|December 24, 2013
PubMed

Insights

Metabotropic glutamate receptor type 5 (mGluR5) does not appear to influence methamphetamine-induced behavioral sensitization. High doses of fenobam, an mGluR5 negative allosteric modulator, caused nonspecific behavioral inhibition in rats.

Area of Science:

  • Neuroscience
  • Pharmacology

Background:

  • Methamphetamine abuse is a significant public health concern.
  • Behavioral sensitization to methamphetamine is a key factor in addiction.
  • Metabotropic glutamate receptor type 5 (mGluR5) is implicated in various neurological processes.

Purpose of the Study:

  • To investigate the role of mGluR5 in the development of methamphetamine-induced behavioral sensitization.
  • To determine if modulating mGluR5 activity affects methamphetamine-induced locomotion.

Main Methods:

  • Sprague-Dawley rats received repeated methamphetamine injections.
  • Locomotor activity was assessed following a methamphetamine challenge dose.
  • Rats were pretreated with mGluR5 modulators (CDPPB, fenobam) or vehicle before the challenge test.

Main Results:

  • Neither CDPPB (positive allosteric modulator) nor fenobam (negative allosteric modulator) altered the expression of methamphetamine-induced behavioral sensitization.
  • A high dose of fenobam (30 mg/kg) significantly decreased methamphetamine-induced locomotion.
  • This decrease in locomotion by high-dose fenobam suggests nonspecific behavioral inhibition.

Conclusions:

  • mGluR5 does not appear to play a significant role in the expression of methamphetamine-induced behavioral sensitization.
  • High doses of fenobam may exert their effects through mechanisms independent of mGluR5 modulation.
  • Further research is needed to elucidate the precise role of mGluR5 in psychostimulant addiction.

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