migraines

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

Lanepitant 2HCl is a non-peptide neurokinin-1 receptor antagonist with analgesic and anti-inflammatory activity.Lanepitant 2HCl inhibits the binding of Substance P to the neurokinin-1 receptor, inhibits neurogenic inflammation and pain transmission, and can be used in the study of painful neuropathic disorders, such as migraines.

Sumatriptan (GR 43175 free base) is an orally active and potent 5-hydroxytryptamine 1 (5-HT1) receptor agonist that crosses the blood-brain barrier and has anti-inflammatory activity with high affinity for 5-HT1D, 5-HT1B, and 5-HT1F receptors for use in acute migraines and acute myocardial infarction.

Eletriptan, second-generation triptans used to treat migraines, is used as an abortion drug.

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

Raseglurant (ADX-10059) is an mGlu5 negative allosteric modulator. It effectively counters migraines and alleviates haloperidol-induced catalepsy in mice.

CGRP Antagonist 6 (Compound 23) is a potent CGRP receptor antagonist (Ki: 0.84 nM). It is utilized in the study of migraines.

Avitriptan is a 5-HT1B/1D receptor agonist with pKi values of 7.44 for 5-HT1Brat, 7.68 for 5-HT1Bhuman, and 8.36 for 5-HT1Dhuman. It can induce contraction in isolated coronary arteries and is used for the treatment of migraines.

Lomerizine, a blocker of diphenylmethylpiperazine Ca2+ channel, is used to prevent migraines.

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

Indomethacin sodium hydrate is an effective orally active, competitive, and reversible inhibitor of COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. It possesses anti-inflammatory, anticancer, and antimicrobial activities and is commonly used in research related to cancer, inflammation, and viral infections. Additionally, it can induce migraines and gastrointestinal injury and is used to study increased intracranial pressure secondary to severe traumatic brain injury in adults, as well as rheumatoid arthritis. It can also be used to induce gastric ulcer models.

BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain.

Donitriptan Mesylate, a 5-HT1B/1D agonist, is used potentially for the treatment of migraines.

Rimegepant, also known as BMS-927711 and BHV-3000, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraines. Rimegepant has shown in vivo efficacy without vasoconstriction effect. BMS-927711 is superior to placebo at several different doses (75 mg, 150 mg, and 300 mg) and has an excellent tolerability profile.

Metoprolol is a selective β1 receptor blocker medication. It is used to treat high blood pressure, chest pain due to poor blood flow to the heart, and a number of conditions involving an abnormally fast heart rate. It is also used to prevent further heart problems after myocardial infarction and to prevent headaches in those with migraines.

Galcanezumab is a humanized IgG4 monoclonal antibody targeting the CGRP ligand, which binds to the ligand calcitonin gene-related peptide. Galcanezumab can be used to prevent and treat migraines or cluster headaches.