5-ht,migraine

Sumatriptan succinate (GR 43175), a serotonin1 (5-HT1) receptor agonist, is used in the acute treatment of a migraine headache.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

Rizatriptan benzoate (MK-462 Benzoate) selectively binds to and activates serotonin (5-HT) 1B receptors and 5-HT 1D receptors providing relief of migraine headaches.

Frovatriptan succinate hydrate (Frova) is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.

NXN-188 is a novel dual-action small molecule compound that combines inhibition of neuronal nitric oxide synthase (nNOS) with 5-HT receptor agonism and is currently in development for the treatment of acute migraine.

Oxetorone fumarate is a non-selective, orally active antagonist of serotonin and 5-HT receptors, exhibiting mild antihistamine and antiadrenergic properties, used for migraine treatment.

Frovatriptan is a highly potent agonist of the 5-HT 1B//D receptors, exhibiting the highest potency among triptan compounds. It possesses prominent cerebroselectivity. Frovatriptan demonstrates efficacy and even superiority in certain endpoints, including when administered during the headache phase of migraine attacks accompanied by aura [1].

Naratriptan Hydrochloride is the hydrochloride salt form of naratriptan, a sulfonamide with selective serotonin (5-HT) 1 receptor agonistic activity and anti-migraine property. Naratriptan hydrochloride (GR-85548A hydrochloride) binds selectively and with high affinity to the 5-HT1D and 5-HT1B receptor subtypes. Activation of these 5-HT1D/B receptors located on intracranial blood vessels leads to vasoconstriction and provides relief of migraine headaches. Naratriptan hydrochloride may also exerts its effect by stimulation of 5-HT1D/1B receptors on sensory nerve endings in the trigeminal system thereby decreasing the release of pro-inflammatory neuropeptides.

Almotriptan hydrochloride, a selective agonist of the 5-HT 1B/1D receptor, is used in the study of migraine attacks [1].