sulfonamide serotonin agonist and vasoconstrictor that acts selectively at 5HT1 receptors; frequently used in treating migraines.
Definition (MSH)
A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
Definition (NCI)
A sulfonamide triptan with vasoconstrictor activity. Sumatriptan selectively binds to and activates serotonin 5-HT1D receptors in the central nervous system (CNS), thereby constricting cerebral blood vessels. This may lead to a relief in pain from vascular headaches. Sumatriptan may also relieve vascular headaches by decreasing the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during a migraine, by reducing extravasation of plasma proteins, and by decreasing the release of other mediators of inflammation from the trigeminal nerve.
Concepts
Organic Chemical (T109)
, Pharmacologic Substance (T121)
A member of the triptan class agents with anti-migraine property. Zolmitriptan selectively binds to and activates serotonin (5-HT) 1B expressed in intracranial arteries and 5_HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei. Receptor binding results in constriction of cranial vessels, reduction of the vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relief migraine headaches by inhibition pro-inflammatory neuropeptide release.
Concepts
Organic Chemical (T109)
, Pharmacologic Substance (T121)