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Eletriptan

Names

[ CAS No. ]:
143322-58-1

[ Name ]:
Eletriptan

[Synonym ]:
3-{[(2R)-1-Methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole
3-{[(2R)-1-Methyl-2-pyrrolidinyl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole
Eletriptan
MFCD00943792
1H-Indole, 3-[[(2R)-1-methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-
5-[2-(benzenesulfonyl)ethyl]-3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-1H-indole

Biological Activity

[Description]:

Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1B Receptor:8.0 (pKi)

5-HT1D Receptor:8.9 (pKi)


[In Vivo]

Eletriptan (10, 30, 100, 300 and 1000 µg/kg; i.v.) reduces total carotid blood flow in anaesthetised pigs by selectively reducing carotid arteriovenous anastomotic blood flow and increasing nutrient blood flow within the carotid vascular bed[2].

[References]

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

[2]. Willems E, et al. 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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
613.4±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H26N2O2S

[ Molecular Weight ]:
382.519

[ Flash Point ]:
324.8±31.5 °C

[ Exact Mass ]:
382.171509

[ PSA ]:
61.55000

[ LogP ]:
3.08

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.634

[ Storage condition ]:
Hygroscopic, Refrigerator, Under Inert Atmosphere

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds