Yohimbine is a 5-HT1A agonist in rats in doses exceeding 1mg/kg.

Dmitry V. Zaretsky, Maria V. Zaretskaia, Joseph A. DiMicco, Daniel E. Rusyniak

Research output: Contribution to journalArticle

13 Scopus citations


Yohimbine is a prototypical alpha2-adrenergic receptor antagonist. Due to its relatively high selectivity, yohimbine is often used in experiments whose purpose is to examine the role of these receptors. For example, yohimbine has been employed at doses of 1-5mg/kg to reinstate drug-seeking behavior after extinction or to antagonize general anesthesia, an effects presumably being a consequence of blocking alpha2-adrenergic receptors. In this report we characterized dose-dependent autonomic and behavioral effects of yohimbine and its interaction with an antagonist of 5-HT<inf>1A</inf> receptors, WAY 100,635. In low doses (0.5-2mg/kg i.p.) yohimbine induced locomotor activation which was accompanied by a tachycardia and mild hypertension. Increasing the dose to 3-4.5mg/kg reversed the hypertension and locomotor activation and induced profound hypothermia. The hypothermia as well as the suppression of the locomotion and the hypertension could be reversed by the blockade of 5-HT<inf>1A</inf> receptors with WAY 100635. Our data confirm that yohimbine possesses 5-HT<inf>1A</inf> properties, and demonstrated that in doses above 1mg/kg significantly activate these receptors.

Original languageEnglish (US)
Pages (from-to)215-219
Number of pages5
JournalNeuroscience Letters
StatePublished - Oct 8 2015


  • 5-HT1A receptors
  • Body temperature
  • Locomotor activity
  • Yohimbine

ASJC Scopus subject areas

  • Neuroscience(all)

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