The effects of 5-HT1A, 5-HT1B and 5-HT1D receptor agonists on trigeminal nociceptive neurotransmission in anaesthetized rats. 1998

M J Cumberbatch, and R G Hill, and R J Hargreaves
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Center, Harlow, Essex, UK.

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.

UI MeSH Term Description Entries
D008297 Male Males
D008881 Migraine Disorders A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1) Acute Confusional Migraine,Headache, Migraine,Status Migrainosus,Abdominal Migraine,Cervical Migraine Syndrome,Hemicrania Migraine,Migraine,Migraine Headache,Migraine Variant,Sick Headache,Abdominal Migraines,Acute Confusional Migraines,Cervical Migraine Syndromes,Disorder, Migraine,Disorders, Migraine,Headache, Sick,Headaches, Migraine,Headaches, Sick,Hemicrania Migraines,Migraine Disorder,Migraine Headaches,Migraine Syndrome, Cervical,Migraine Syndromes, Cervical,Migraine Variants,Migraine, Abdominal,Migraine, Acute Confusional,Migraine, Hemicrania,Migraines,Migraines, Abdominal,Migraines, Acute Confusional,Migraines, Hemicrania,Sick Headaches,Variant, Migraine,Variants, Migraine
D010080 Oxazoles Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions. Oxazole,1,3-Oxazolium-5-Oxides,Munchnones,1,3 Oxazolium 5 Oxides
D011725 Pyridines Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
D011758 Pyrroles Azoles of one NITROGEN and two double bonds that have aromatic chemical properties. Pyrrole
D011985 Receptors, Serotonin Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action. 5-HT Receptor,5-HT Receptors,5-Hydroxytryptamine Receptor,5-Hydroxytryptamine Receptors,Receptors, Tryptamine,Serotonin Receptor,Serotonin Receptors,Tryptamine Receptor,Tryptamine Receptors,Receptors, 5-HT,Receptors, 5-Hydroxytryptamine,5 HT Receptor,5 HT Receptors,5 Hydroxytryptamine Receptor,5 Hydroxytryptamine Receptors,Receptor, 5-HT,Receptor, 5-Hydroxytryptamine,Receptor, Serotonin,Receptor, Tryptamine,Receptors, 5 HT,Receptors, 5 Hydroxytryptamine
D004558 Electric Stimulation Use of electric potential or currents to elicit biological responses. Stimulation, Electric,Electrical Stimulation,Electric Stimulations,Electrical Stimulations,Stimulation, Electrical,Stimulations, Electric,Stimulations, Electrical
D000200 Action Potentials Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli. Spike Potentials,Nerve Impulses,Action Potential,Impulse, Nerve,Impulses, Nerve,Nerve Impulse,Potential, Action,Potential, Spike,Potentials, Action,Potentials, Spike,Spike Potential
D000700 Analgesics Compounds capable of relieving pain without the loss of CONSCIOUSNESS. Analgesic,Anodynes,Antinociceptive Agents,Analgesic Agents,Analgesic Drugs,Agents, Analgesic,Agents, Antinociceptive,Drugs, Analgesic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

M J Cumberbatch, and R G Hill, and R J Hargreaves
July 1995, European journal of pharmacology,
M J Cumberbatch, and R G Hill, and R J Hargreaves
June 1989, Naunyn-Schmiedeberg's archives of pharmacology,
M J Cumberbatch, and R G Hill, and R J Hargreaves
September 1995, No to shinkei = Brain and nerve,
M J Cumberbatch, and R G Hill, and R J Hargreaves
April 1990, Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology,
M J Cumberbatch, and R G Hill, and R J Hargreaves
April 2007, Neuroscience letters,
M J Cumberbatch, and R G Hill, and R J Hargreaves
December 2008, Brain : a journal of neurology,
M J Cumberbatch, and R G Hill, and R J Hargreaves
June 1990, European journal of pharmacology,
Copied contents to your clipboard!