Eletriptan-d5

Names

[ CAS No. ]:
1126745-65-0

[ Name ]:
Eletriptan-d5

[Synonym ]:
Eletriptan-d5

Biological Activity

[Description]:

Eletriptan-d5 is the deuterium labeled Eletriptan[1]. 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[2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  

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

[3]. 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 Aug358(2):212-9.  

Chemical & Physical Properties

[ Molecular Formula ]:
C22H21D5N2O2S

[ Molecular Weight ]:
387.55000

[ Exact Mass ]:
387.20300

[ PSA ]:
61.55000

[ LogP ]:
4.83970

Related Compounds