Eletriptan (10, 30, 100, 300 and 1000 µg/kg; iv) reduces total carotid blood flow in anesthetized pigs by selectively reducing carotid arteriovenous anastomotic blood flow and boosting nutritive blood flow within the carotid vascular bed [ 2].

Absorption, Distribution and Excretion
Electriptan is well absorbed after oral administration, with an average absolute bioavailability of approximately 50%. 138 L Renal clearance = 3.9 L/h Metabolism/Metabolites In vitro studies have shown that eletriptan is primarily metabolized by the cytochrome P-450 enzyme CYP3A4. The N-demethylated metabolite of eletriptan is currently the only known active metabolite. Biological Half-Life The terminal elimination half-life of eletriptan is approximately 4 hours.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited information suggests that with mothers taking up to 80 mg of eletriptan daily, the drug concentration in breast milk is low and is not expected to have any adverse effects on breastfed infants. Nipple pain, burning sensation, and breast pain have been reported after taking sumatriptan and other triptans. This is sometimes accompanied by a decrease in milk production.
◉ Effects on Breastfed Infants
No relevant published information was found as of the revision date.
◉ Effects on Lactation and Breast Milk
A review of four European adverse reaction databases found 26 reports of nipple pain, burning sensation, breast pain, breast engorgement, and/or let-down pain in breastfeeding women taking triptans. The pain was sometimes severe and occasionally led to a decrease in milk production. The pain usually subsides gradually as the drug is metabolized. The authors suggest that triptans may cause vasoconstriction in the arteries surrounding the breast, nipple, mammary alveoli, and ducts, leading to pain and the painful milk ejection reflex.

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Protein Binding
Plasma protein binding is moderate, approximately 85%.

[1]. McCormack PL, Keating GM. Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-49.

[2]. Porcine carotid vascular effects of eletriptan (UK-116,044): a new 5-HT1B/1D receptor agonist with anti-migraine activity. Naunyn Schmiedebergs Arch Pharmacol. 1998 Aug;358(2):212-9.

Eletriptan is an N-alkylpyrrolidine compound, specifically N-methylpyrrolidine, in which the pro-R hydrogen at the 2-position is replaced by {5-[2-(benzenesulfonyl)ethyl]-1H-indol-3-yl}methyl. It is a serotonergic agonist, vasoconstrictor, and nonsteroidal anti-inflammatory drug. It belongs to the indole, N-alkylpyrrolidine, and sulfone classes. It is the conjugate base of eletriptan (1+). Eletriptan is a second-generation triptan developed by Pfizer for the treatment of migraines. Eletriptan is a 5-hydroxytryptamine-1b and 5-hydroxytryptamine-1d receptor agonist. Its mechanism of action is as a 5-hydroxytryptamine-1b and 5-hydroxytryptamine-1d receptor agonist. See also: eletriptan hydrobromide (in salt form); eletriptan hydrobromide monohydrate (active ingredient). Drug Indications For the treatment of acute migraine with or without aura in adults. FDA Label Mechanism of Action Eletriptan has high affinity for 5-HT1B, 5-HT1D, and 5-HT1F receptors, moderate affinity for 5-HT1A, 5-HT1E, 5-HT2B, and 5-HT7 receptors, and very low or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A, and 5-HT6 receptors. In contrast, eletriptan has no significant pharmacological activity against adrenergic α1, α2, or β receptors; dopaminergic D1 or D2 receptors; muscarinic receptors; or opioid receptors. While the complete mechanism of action of 5-HT receptor agonists in relieving migraines is not fully elucidated, some studies suggest that activation of 5-HT1 receptors located on intracranial blood vessels can lead to vasoconstriction, thereby relieving migraines. Other studies suggest that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal nerve system can inhibit the release of pro-inflammatory neuropeptides.
Pharmacodynamics
Eletriptan is a selective serotonin 1B/1D receptor agonist.
In anesthetized dogs, eletriptan has been shown to reduce carotid artery blood flow, causing only a slight increase in arterial blood pressure even at high doses. Although its effect on blood flow is limited to the carotid bed, a decrease in coronary artery diameter has also been observed. Eletriptan has also been shown to inhibit trigeminal nerve activity in rats.

382.52

382.171

143322-58-1

Eletriptan hydrobromide;177834-92-3;Eletriptan-d3;1287040-94-1;Eletriptan-d5;1126745-65-0;Eletriptan-d5 hydrochloride

77993

Typically exists as solid at room temperature

1.2±0.1 g/cm3

613.4±55.0 °C at 760 mmHg

324.8±31.5 °C

0.0±1.8 mmHg at 25°C

1.634

3.08

1

3

6

27

582

1

CN1CCC[C@@H]1CC2=CNC3=C2C=C(C=C3)CCS(=O)(=O)C4=CC=CC=C4

PWVXXGRKLHYWKM-LJQANCHMSA-N

InChI=1S/C22H26N2O2S/c1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3/t19-/m1/s1

5-[2-(benzenesulfonyl)ethyl]-3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-1H-indole

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)