Migraine

Rimegepant (BMS-927711; BHV-3000) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC₅₀ of 8.01 and a K_i of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .

Galcanezumab (LY 2951742) is a humanized IgG4 monoclonal antibody against the CGRP ligand. Galcanezumab can be used for migraine or cluster headaches research.

Erenumab (AMG-334) is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene-related peptide (CGRP) receptor. Erenumab prevents the increase in dermal blood flow in cynomolgus monkeys. Erenumab can be used in the research of episodic migraine.

Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A). Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury.

Eptinezumab (ALD-403) is a human monoclonal antibody targeting the α and β subtypes of human calcitonin gene-related peptide (CGRP). Eptinezumab binds to the CGRP ligand and blocks its binding to endogenous CGRP receptors, thereby inhibiting receptor activation. Eptinezumab can be used in research related to migraine.

Phenopyrazone (Diphenox), a derivative of Antipyrine (HY-B0171), exhibits oral activity as well as analgesic, antipyretic, anti-inflammatory, and antidiarrheal properties. Phenopyrazone can be used in research related to headache, rheumatism, chronic diarrhea and varicose veins.

5-HT2A receptor agonist-14 (Compound I-23) is a tricyclic 5-HT2A receptor agonist with a pEC₅₀ value ≥ 6. 5-HT2A receptor agonist-14 can be used in research related to depression, anxiety, substance abuse and headache.

BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABA_A receptor (GABA_A receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na⁺ channels (K_i = 350 μM) and NMDA receptors (NMDA receptor) (IC₅₀ = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.

Rimegepant (BMS-927711) sulfate hydrate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 0.027 nM and an IC₅₀ of 0.14 nM for hCGRP receptor. Rimegepant sulfate hydrate can be used for migraine research.

Vinyl-L-NIO (L-VNIO) hydrochloride is a neuronal nitric oxide synthase (NOS) inhibitor with a rat K_i of 0.10 μM. Vinyl-L-NIO hydrochloride inhibits NADPH oxidase activity, attenuates renal fibrosis, inflammation, oxidative stress indices, and albuminuria. Vinyl-L-NIO hydrochloride can be used for the research of parkinson's disease, migraine headache, and hypertension.

Lerimazoline is a selective 5-HT1D receptor agonist with K_i values of 72 and 3480 nM for h5-HT1D and h5-HT1B. Lerimazoline inhibits Forskolin (HY-15371)-stimulated cAMP production and induces contractions in rabbit saphenous vein preparations. Lerimazoline can be used for the research of migraine.

Nicotinanilide (N-Phenylnicotinamide) (Compound 12) is an aquaporin 4 (AQP4) inhibitor. Nicotinanilide can be used for research on diseases associated with AQP4 dysfunction, such as epilepsy and migraine.

O-1812 is a selective CB₁ ligand. O-1812 is also a very weak AMT inhibitor. O-1812 can be used in the research of chronic pain, migraines, and inflammation.

PCC0105005 is a dual-target CGRP Receptor antagonist (IC₅₀ = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC₅₀ = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine.

Rimegepant (BMS-927711) hemisulfate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 0.027 nM and an IC₅₀ of 0.14 nM for hCGRP receptor. Rimegepant hemisulfate can be used for migraine research.

Valproic acid magnesium (Magnesium valproate) is an orally active HDAC inhibitor, with IC₅₀ in the range of 0.5 and 2 mM. Valproic acid magnesium inhibits HDAC1 (IC₅₀, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid magnesium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid magnesium is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

Dihydroergotamine (DFN-19) is a BBB-permeable and semisynthetic, hydrogenated ergot alkaloid. Dihydroergotamine can cause vasoconstriction by stimulating alpha-adrenergic and 5-HT_2A receptors. Dihydroergotamine can be used in the research of migraine.

Iprazochrome is a serotonin antagonist. Iprazochrome can be used in prophylaxis of migraine.

UK-315716 is an NMDA receptor antagonist. UK-315716 has a synergistic neuroprotective effect. UK-315716 can be used for research on neurological diseases such as stroke and headache.

Rizatriptan (MK 462 free base) is an orally active 5-HT_1B/5-HT_1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache.