Eletriptan HCl
Eletriptan hydrobromide
CAS: 177834-92-3
Molecular Formula: C22H26N2O2S
Eletriptan HCl - Names and Identifiers
Eletriptan HCl - Physico-chemical Properties
| Molecular Formula | C22H26N2O2S |
| Molar Mass | 382.51904 |
| Melting Point | 169-171?C |
| Boling Point | 633.9℃ at 760 mmHg |
| Solubility | DMSO 93 mg/mL Water <1 mg/mL Ethanol <1 mg/mL ; Soluble in DMSO (100 mM), methanol |
| Appearance | Morphological powder, color off-white to light tan |
| Color | off-white to light tan |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Sensitive | Sensitive to heat and light |
| Use | A selective SR-1B/SR-1D |
| In vitro study | [Eletriptan causes concentration-dependent contraction of the middle meningeal artery, coronary artery, and saphenous vein. Electriptan is more potent in the middle meningeal artery than in the coronary artery (86 times), or in the saphenous vein (66 times). Observed in clinical trials, Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at maximum free plasma concentrations (C(max)) the lower-induced predictable contractions were similar in the middle meningeal artery. |
| In vivo study | Electriptan (<1000 mg/kg, I. V.) dose-dependently reduced carotid blood flow in anesthetized dogs. Eletriptan reduced the diameter of the coronary arteries with an ED50 value of 63 mg/kg in anesthetized dogs. In Dural rats, administration of Eletriptan (<300 mg/kg, I. V.) prior to electrical Trigeminal stimulation resulted in complete inhibition of dose-related plasma protein extravasation. In brain dura mater rats, Eletriptan (100 mg/kg, I. V.) completely inhibited plasma protein extravasation. In Head Pain patients, 2 hours after administration, the Head Pain response rate in the placebo group was 24%; Eletriptan (20 mg) was 54% ;Eletriptan (40 mg) was 65%; eletriptan (80 mg) was 77%. Eletriptan was well tolerated, and in migraine patients, the major adverse effects were mild or moderate in intensity and were transient. In cats, the iontophoresis effluent (50 nA) of electriptan inhibited the response of 75% of cells and inhibited an average of 42% of cell discharges. |
Eletriptan HCl - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| HS Code | 29339900 |
Eletriptan HCl - Upstream Downstream Industry
Eletriptan HCl - Introduction
Eletriptan HBr is a selective serotonin 1B and 1D receptor agonist with Ki values of 0.92 nM and 3.14 nM, respectively.
Last Update：2022-10-16 17:30:53
Eletriptan HCl - Uses and synthesis methods
biological activity
Eletriptan (UK-116044) is a selective serotonin 1B and 1D receptor agonist with Ki values of 0.92 nM and 3.14 nM, respectively.
target
Target Value
5-HT1B 0.92 nM(Ki)
5-HT1D 3.14 nM(Ki)
in vitro study
[ Eletriptan causes concentration-dependent contraction of the middle meningeal artery, coronary artery and saphenous vein. Eletriptan were more potent in the middle meningeal artery than in the coronary artery (86-fold), or in the saphenous vein (66-fold). Predictable contractions induced by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at maximal free plasma concentrations (C(max)) were observed in clinical trials to be similar in the middle meningeal artery.
in vivo studies
In anesthetized dogs, Eletriptan (<1000 mg/kg, intravenous injection) reduced carotid blood flow dose-dependently. Eletriptan reducing the diameter of coronary arteries, the ED50 value in anesthetized dogs is 63 mg/kg. In cerebral dural rats, Eletriptan (<300 mg/kg, intravenous) administration before electrical stimulation of the trigeminal ganglion will produce complete inhibition of dose-related plasma protein extravasation. In cerebral dural rats, Eletriptan (100 mg/kg, intravenous injection) completely inhibited plasma protein extravasation. In migraine patients, 2 hours after administration, the headache response rate in the comfort group was 24%; Eletriptan (20 mg) was 54% ;Eletriptan (40 mg) was 65%; and Eletriptan (80 mg) was 77%. The Eletriptan is well tolerated. In migraine patients, the main adverse reactions are mild or moderate intensity and are transient. In cats, Eletriptan iontophoresis discharge (50 nA) inhibited the response of 75% cells and inhibited the average 42% cell discharge.
Last Update：2024-04-10 22:29:15
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CAS: 177834-92-3
Tel: 18301782025
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Multiple SpecificationsSpot supply
Product Name: Eletriptan HBr; UK-116044 hydrobromide Visit Supplier Webpage Request for quotationCAS: 177834-92-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: Eletriptan hydrobromide Visit Supplier Webpage Request for quotationCAS: 177834-92-3
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185
Wechat: chinaskyrun
Spot supply
Product Name: Eletriptan hydrobromide Visit Supplier Webpage Request for quotationCAS: 177834-92-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: Eletriptan HBr Visit Supplier Webpage Request for quotationCAS: 177834-92-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: Eletriptan HBr Visit Supplier Webpage Request for quotation
CAS: 177834-92-3
Tel: 18301782025
Email: 3008007409@qq.com
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QQ: 3008007409
CAS: 177834-92-3
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View History
Eletriptan HCl
(2S)-6-AMINO-2-[[(2S)-2-AMINO-5-(DIAMINOMETHYLIDENEAMINO)PENTANOYL]AMINO]HEXANOIC ACID
甘油三乙酰羟基硬脂酸酯
甲基4-羟基丁酸酯
溶血磷脂酰胆碱(牛脑)
N-(FMOC-5-AMINO-3-OXA-PENTYL)-SUCCINAMIC ACID
2-四氢吡喃酸
4,5-DIMETHYL-1H-IMIDAZOLE(游离碱)
HEPTYL CHLOROFORMATE
Methyl 2-aMino-3-Methylbe...
(2S)-6-AMINO-2-[[(2S)-2-AMINO-5-(DIAMINOMETHYLIDENEAMINO)PENTANOYL]AMINO]HEXANOIC ACID
甘油三乙酰羟基硬脂酸酯
甲基4-羟基丁酸酯
溶血磷脂酰胆碱(牛脑)
N-(FMOC-5-AMINO-3-OXA-PENTYL)-SUCCINAMIC ACID
2-四氢吡喃酸
4,5-DIMETHYL-1H-IMIDAZOLE(游离碱)
HEPTYL CHLOROFORMATE
Methyl 2-aMino-3-Methylbe...
Raw Materials for Eletriptan HCl
Hydrogen bromide
Triethylamine
Palladium hydroxide
interMediates of eletriptan hydrobroMide
(R)-5-BROMO-3-[(1-METHYL-2-PYRROLIDINYL)METHYL]-1H-INDOLE
Triethylamine
Palladium hydroxide
interMediates of eletriptan hydrobroMide
(R)-5-BROMO-3-[(1-METHYL-2-PYRROLIDINYL)METHYL]-1H-INDOLE