Eletriptan HBr: Key Facts, Uses & Research FAQ
Eletriptan HBr: Key Facts, Uses & Research FAQ
Eletriptan HBr is a selective serotonin 5-HT1B/1D receptor agonist of the triptan class, widely used in pharmacological research to investigate migraine pathophysiology and craniovascular serotonergic signaling.
- Chemical Name
- (R)-3-[(1-Methylpyrrolidin-2-yl)methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole hydrobromide
- Molecular Formula
- C22H26N2O2S · HBr
- Primary Target
- Serotonin 5-HT1B and 5-HT1D receptors (selective agonist)
- Therapeutic/Research Class
- Triptan; antimigraine agent; serotonin receptor agonist
- Recommended Storage
- Store at 2–8 °C, protected from light and moisture
- Aladdin SKU
- E129729
What Is Eletriptan HBr and How Does It Work?
Eletriptan HBr (eletriptan hydrobromide) is the hydrobromide salt form of eletriptan, a second-generation triptan compound. It acts as a selective agonist at serotonin 5-HT1B and 5-HT1D receptors, which are expressed on cranial blood vessels and trigeminal sensory neurons. Activation of these receptors produces two key pharmacological effects relevant to migraine research: vasoconstriction of dilated intracranial vessels and inhibition of pro-inflammatory neuropeptide release (e.g., calcitonin gene-related peptide, CGRP) from trigeminal nerve terminals.
In the research setting, Eletriptan HBr is used as a tool compound to dissect serotonergic signaling pathways involved in vascular tone regulation and pain modulation. Its high selectivity for 5-HT1B/1D over other serotonin receptor subtypes makes it a valuable pharmacological probe in receptor characterization and functional assay development.
Physicochemical Properties and Formulation Guidance
Eletriptan HBr is a white to off-white crystalline powder. As the hydrobromide salt, it exhibits enhanced aqueous solubility compared to the free base, which is advantageous for preparing stock solutions for in vitro assays. The compound is generally soluble in water and DMSO; researchers should verify solubility empirically for their specific buffer systems and concentration requirements.
Recommended stock solution preparation: Dissolve in sterile water or phosphate-buffered saline (PBS) at physiological pH for aqueous assays. For DMSO stock solutions, prepare at ≥10 mM and store in single-use aliquots at −20 °C to minimize freeze-thaw degradation. Avoid prolonged exposure to light and moisture during handling. Filter-sterilize aqueous solutions through a 0.22 µm membrane before use in cell-based assays.
Note: Specific solubility values and molecular weight should be confirmed against the certificate of analysis (CoA) provided with each lot.
Handling, Storage, and Safety Considerations
Storage: Store Eletriptan HBr at 2–8 °C in a tightly sealed container, protected from light and moisture. Long-term archival aliquots may be stored at −20 °C. Allow the container to equilibrate to room temperature before opening to prevent condensation on the solid material.
Handling precautions: As with all research chemicals, handle with appropriate personal protective equipment (PPE) including nitrile gloves, lab coat, and safety glasses. Work in a well-ventilated area or fume hood when weighing the powder. Avoid inhalation of dust and contact with skin and eyes. Eletriptan HBr is intended for research use only and is not approved for human or veterinary therapeutic administration in a research-reagent context.
Disposal: Dispose of waste material in accordance with local institutional and governmental regulations for pharmaceutical compounds. Consult your institution's Environmental Health and Safety (EHS) office for guidance.
Research Applications and Experimental Considerations
Eletriptan HBr is employed across a range of in vitro and in vivo research paradigms:
- Receptor binding and competition assays: Used to characterize 5-HT1B and 5-HT1D receptor affinity and selectivity profiles in radioligand displacement studies.
- Functional cAMP assays: As a Gi-coupled receptor agonist, eletriptan reduces forskolin-stimulated cAMP accumulation; this can be quantified using HTRF, ELISA, or luminescence-based assay kits.
- Vascular pharmacology: Applied in isolated vessel preparations to study vasoconstrictor responses mediated by 5-HT1B receptors.
- Trigeminal pain models: Used in preclinical in vivo models to investigate trigeminovascular activation and CGRP release.
- Transporter and metabolic studies: Useful as a reference compound in CYP3A4 metabolism studies, given eletriptan's known metabolic pathway.
Researchers should include appropriate vehicle controls (matched solvent at equivalent concentration) and reference agonists/antagonists in all experimental designs to ensure data validity.
Frequently asked questions
What is the difference between eletriptan free base and Eletriptan HBr?
Eletriptan HBr is the hydrobromide salt form of eletriptan, which offers improved aqueous solubility and stability compared to the free base form. When preparing molar concentrations for assays, researchers must account for the molecular weight of the HBr salt rather than the free base. The pharmacological activity at 5-HT1B/1D receptors is attributable to the eletriptan moiety itself.
How should I prepare a working solution of Eletriptan HBr for cell-based assays?
Prepare a concentrated stock solution (e.g., 10–50 mM) by dissolving Eletriptan HBr in sterile water or DMSO and store in single-use aliquots at −20 °C. On the day of the experiment, dilute the stock into the appropriate assay buffer or cell culture medium to achieve the desired working concentration, keeping the final DMSO concentration below 0.1% (v/v) to avoid cytotoxic effects. Always filter-sterilize aqueous solutions through a 0.22 µm membrane before adding to cells.
Which receptor subtypes does Eletriptan HBr target, and are there any off-target activities to consider?
Eletriptan HBr primarily targets 5-HT1B and 5-HT1D receptors with high selectivity. Some literature reports indicate measurable affinity for 5-HT1F and, to a lesser extent, 5-HT2B receptors at higher concentrations, which may be relevant in high-dose experimental designs. Researchers are advised to include appropriate selectivity controls and consult current pharmacological profiling literature when interpreting results.
What are the recommended storage conditions to maintain the stability of Eletriptan HBr?
Eletriptan HBr should be stored at 2–8 °C in a tightly closed container away from light and moisture for routine use. For long-term storage, aliquots may be kept at −20 °C. To prevent moisture absorption, allow the container to reach room temperature before opening. Refer to the certificate of analysis for lot-specific stability data.
Is Eletriptan HBr (SKU E129729) available from Aladdin Scientific, and how can I order it?
Yes, Eletriptan HBr is available from Aladdin Scientific under SKU E129729. You can place an order through the Aladdin Scientific website, by contacting your local sales representative, or via your institution's procurement system. For bulk quantities or custom packaging inquiries, please contact Aladdin's customer service team directly.
References
- Villalón CM, Tfelt-Hansen P. Eletriptan. In: Olesen J, et al., eds. The Headaches. 3rd ed. Lippincott Williams & Wilkins; 2006.
- Jhee SS, et al. Eletriptan: pharmacokinetics and pharmacodynamics. Clin Pharmacokinet. 2001.
- Sanford M, Carey P. Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2010.
Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
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