The effects of 5-HT1A, 5-HT1B and 5-HT1D receptor agonists on trigeminal nociceptive neurotransmission in anaesthetized rats

Eur J Pharmacol. 1998 Nov 27;362(1):43-6. doi: 10.1016/s0014-2999(98)00764-x.


Pre-clinical studies have suggested that one mechanism of antimigraine action of the 'triptan' 5-HT1B/1D receptor agonists may be through inhibition of central nociceptive transmission in the trigeminal dorsal horn. In anaesthetized rats, the 5-HT1B/1D receptor agonist, zolmitriptan (up to 3 mg kg(-1), i.v.), inhibited the action potential discharge of single trigeminal neurones to noxious electrical stimulation of the middle meningeal artery. In contrast, the selective 5-HT1B receptor agonist, CP-93,129 (3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one), and the 5-HT1A receptor selective agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) had no effect in this assay at up to 3 mg kg(-1), i.v.. Brain penetrant, triptan 5-HT1B/1D receptor agonists may therefore mediate their central trigeminal anti-nociceptive action in the rat via 5-HT1D, but not 5-HT1B or 5-HT1A, receptors.

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
  • Action Potentials / drug effects
  • Analgesics / pharmacology
  • Animals
  • Electric Stimulation
  • Male
  • Migraine Disorders / drug therapy
  • Oxazoles / pharmacology*
  • Oxazolidinones*
  • Pyridines / pharmacology
  • Pyrroles / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Serotonin / classification
  • Receptors, Serotonin / drug effects*
  • Serotonin Receptor Agonists / pharmacology*
  • Trigeminal Caudal Nucleus / drug effects*
  • Tryptamines


  • Analgesics
  • Oxazoles
  • Oxazolidinones
  • Pyridines
  • Pyrroles
  • Receptors, Serotonin
  • Serotonin Receptor Agonists
  • Tryptamines
  • 3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo(3,2-b)pyrid-5-one
  • zolmitriptan
  • 8-Hydroxy-2-(di-n-propylamino)tetralin