Eletriptan (hydrobromide)

Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT1B and 5-HT1D receptor agonist with antimigraine activity, with Ki of 0.92 nM and 3.14 nM, respectively[1][2][3][4][5][6].

Product Specifications

CAS Number

[177834-92-3]

Product Name Alternative

Eletriptan HBr; UK-116044 (hydrobromide)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Eletriptan-hydrobromide.html

Purity

99.97

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(CCC1=CC2=C(NC=C2C[C@@H]3N(CCC3)C)C=C1)(C4=CC=CC=C4)=O.Br

Molecular Formula

C22H27BrN2O2S

Molecular Weight

463.43

Precautions

H302, H315, H319, H335

References & Citations

[1]Napier C, et al. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol, 1999, 368 (2-3), 259-268.|[2]MaassenVanDenBrink A, et al. Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels. Neurology, 2000, 55 (10), 1524-1530.|[3]Gupta P, et al. The in vivo pharmacological profile of eletriptan (UK-116,044) : a potent and novel 5-HT (1B/1D) receptor agonist. Eur J Pharmacol, 2000, 398 (1), 73-81.|[4]Hoskin KL, et al. The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res, 2004, 998 (1), 91-99.|[5]Willems E, et al. Porcine carotid vascular effects of eletriptan (UK-116,044) : a new 5-HT1B/1D receptor agonist with anti-migraine activity[J]. Naunyn-Schmiedeberg's archives of pharmacology, 1998, 358: 212-219.|[6]Johnson D E, et al. Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain[J]. European journal of pharmacology, 2001, 425 (3) : 203-210.