| Name | Eletriptan hydrobromide |
| Description | Eletriptan hydrobromide (Eletriptan HBr) is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D [5-HT1B/1D] receptor. |
| In vitro | [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan). [1] Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery. [2] |
| In vivo | The total number of binding sites (Bmax) of [3H]Eletriptan to 5-HT1B and 5-HT1D was 2478 fmol/mg and 1576 fmol/mg, respectively.The binding rate of [3H]Eletriptan (K(on) 0.249/min/nM) was significantly faster than that of [3H]sumatriptan (K(on) 0.024/ min/nM), while the shedding rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan) was significantly slower than [3H]Eletriptan . [1] Eletriptan induces concentration-dependent constriction in meningeal arteries, coronary arteries, and saphenous veins.Eletriptan is more potent in meningeal arteries than in coronary arteries (86-fold) or saphenous veins (66-fold). The predicted contractility of Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C (max) in meningeal arteries observed in clinical trials is similar. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (129.47 mM), Sonication is recommended.
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| Keywords | Inhibitor | Eletriptan Hydrobromide | Eletriptan hydrobromide | Eletriptan | 5-hydroxytryptamine Receptor | UK 116044 | 5-HT Receptor | UK116044 | inhibit | Serotonin Receptor |
| Inhibitors Related | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
