migraine

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

Divalproex Sodium (Valproate semisodium) binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. It also is an HDAC inhibitor, Comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex may also work by suppressing repetitive neuronal firing through the inhibition of voltage-sensitive sodium channels.

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.

A2764 dihydrochloride is a highly selective inhibitor of TWIK-related spinal cord K+ channel (TRESK).

Vazegepant hydrochloride (Vazegepant HCl) is the first intranasal gepant for the acute treatment of migraine and has announced a positive phase II/III study.

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.

LY 344864, a specifc receptor agonist, is an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.

JNJ-17203212 is a potent and selective antagonist of TRPV1 (human TRPV1 and rat TRPV1, IC50 of 65 nM and 102 nM).

Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

Zatosetron maleate(LY 277359 maleate) is a potent and selective serotonin 5HT3 receptor antagonist for the study of acute migraine.

Lanepitant (LY303870) is a nonpeptide neurokinin-1 (NK-1) antagonist with analgesic activity that inhibits neurogenic dura mater inflammation and is used for the prevention of migraine.

BF-1 is a novel selective 5-HT2 receptor antagonist that acts by blocking neurogenic dural plasma protein extravasation induced by mCPP or BW723C86.BF-1 is used in the study of migraine.

LY-2300559 is an agonist of metabotropic glutamate receptor 2 (mGluR2) and can be used in studies about the treatment of migraine.

Dasolampanel (NGX-426) is an orally available ionotropic glutamate receptor AMPA and Kainate receptor antagonist for the study of chronic pain disorders, including neuropathic pain and migraine.

Selurampanel (BGG492) is an orally active and selective competitive AMPA glutamate receptor antagonist, a quinazoline-dione sulfonamide. selurampanel is used in the study of epilepsy, migraine and tinnitus.

Etilefrine pivalate HCl is an orally active compound for the treatment of migraine headaches.

Stacofylline is a xanthine derivative that is used to treat migraine headaches.

Femoxetine hydrochloride is a selective 5-hydroxytryptamine reuptake inhibitor used in the study of migraine, depression and eating disorders.

Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory drug (NSAID) used to treat migraine symptoms.

Flunarizine dihydrochloride (R14950) is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Flunarizine dihydrochloride (R14950) is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

L-5-Hydroxytryptophan (L-5-HTP) is a naturally occurring amino acid and dietary supplement that serves as a precursor to the neurotransmitter serotonin. It can be used as an antidepressant, appetite suppressant, and sleep aid, and acts as an antagonist to reserpine. L-5-HTP is widely used in research on myoclonus, fibromyalgia, migraine, and cerebellar ataxia, and is also commonly used to induce epilepsy models.

Pizotifen (Pizotyline) is a strong serotonin and tryptamine antagonist, with weak anticholinergic, anti-histaminic and anti-kinin effects. It also possesses sedative and appetite-stimulating properties. Pizotifen hydrochloride is an active ingredient in Sandomigran, which is used for the prophylactic management of migraine. Sandomigran is available in number of countries excluding the United States.