eletriptan hydrobromide
Eletriptan hydrobromide
CAS: 177834-92-3
Molecular Formula: C22H26N2O2S
eletriptan hydrobromide - Names and Identifiers
eletriptan hydrobromide - 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 hydrobromide - 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 hydrobromide - Upstream Downstream Industry
eletriptan hydrobromide - 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 hydrobromide - 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
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Product Name: Eletriptan HBr Visit Supplier Webpage Request for quotation
CAS: 177834-92-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 177834-92-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
Raw Materials for eletriptan hydrobromide
Hydrochloric acid
Palladium hydroxide
Palladium (II) Acetate
(R)-pyrrolidine-1,2-dicarboxylic acid 1-phenyl ester
Eletriptan Hydrobromide Monohydrate
3-[((2R)-1-METHYLPYRROLIDIN-2-YL)METHYL]-5-[(E)-2-(PHENYLSULFONYL)VINYL]INDOLE
(R)-N-Acetyl-5-bromo-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole
(R)-5-BROMO-3-[(1-METHYL-2-PYRROLIDINYL)METHYL]-1H-INDOLE
(R)-5-Bromo-3-((1-methylpyrrolidin-2-yl)methyl)-1H-indole
Palladium hydroxide
Palladium (II) Acetate
(R)-pyrrolidine-1,2-dicarboxylic acid 1-phenyl ester
Eletriptan Hydrobromide Monohydrate
3-[((2R)-1-METHYLPYRROLIDIN-2-YL)METHYL]-5-[(E)-2-(PHENYLSULFONYL)VINYL]INDOLE
(R)-N-Acetyl-5-bromo-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole
(R)-5-BROMO-3-[(1-METHYL-2-PYRROLIDINYL)METHYL]-1H-INDOLE
(R)-5-Bromo-3-((1-methylpyrrolidin-2-yl)methyl)-1H-indole