An agonist of 5-HT1B and 5-HT1D receptors; induces vasoconstriction of isolated rabbit common carotid artery rings (pD2 = 4.9); preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1

Eletriptan – 5 mg

Brand:
Cayman
CAS:
143322-58-1
Storage:
-20
UN-No:
Non-Hazardous - /

Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.{32188} It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).{42283} Formulations containing eletriptan have been used in the treatment of migraine headache.  

 

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Description

An agonist of 5-HT1B and 5-HT1D receptors; induces vasoconstriction of isolated rabbit common carotid artery rings (pD2 = 4.9); preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively)

Formal name: 3-[[(2R)-1-methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole

Synonyms:  UK 116044

Molecular weight: 382.5

CAS: 143322-58-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience

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