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Thioperamide, the selective histamine H3 receptor antagonist, attenuates stimulant-induced locomotor activity in the

J Clapham1, G J Kilpatrick

  • 1Department of Pharmacology (2), Glaxo Research & Development Ltd., Ware, Herts., UK.

European Journal of Pharmacology
|July 1, 1994
PubMed

Insights

Histamine H3 receptor antagonist thioperamide inhibits stimulant-induced hyperactivity in mice. This effect was dose-dependent and reversed by the H3 agonist (R)-alpha-methylhistamine, suggesting H3 receptor antagonism modulates locomotor activity.

Area of Science:

  • Neuropharmacology
  • Behavioral Neuroscience

Background:

  • The central histamine H3 receptor regulates neurotransmitter release.
  • Histaminergic modulation of locomotor activity is not fully understood.

Purpose of the Study:

  • To investigate the role of histamine H3 receptors in stimulant-induced locomotor activity.
  • To examine the effects of H3 receptor agonist and antagonist on mouse behavior.

Main Methods:

  • Mice were administered amphetamine, apomorphine, or cocaine to induce hyperactivity.
  • The effects of (R)-alpha-methylhistamine (H3 agonist) and thioperamide (H3 antagonist) on locomotor activity were assessed.
  • Dose-response relationships and interactions between drugs were analyzed.

Main Results:

  • Amphetamine, apomorphine, and cocaine significantly increased locomotor activity.
  • Thioperamide dose-dependently inhibited hyperactivity induced by amphetamine, apomorphine, and cocaine.
  • (R)-alpha-methylhistamine alone did not affect spontaneous activity but reversed thioperamide's inhibitory effect.

Conclusions:

  • Central histamine H3 receptor antagonism inhibits stimulant-induced hyperactivity.
  • The histamine H3 receptor plays a significant role in modulating the effects of common psychostimulants.

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