Home Neuronal Signaling 5-HT Receptor agonist Eletriptan HBr For research use only.

Eletriptan HBr

Synonyms: UK-116044

Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

Eletriptan HBr Chemical Structure

Eletriptan HBr Chemical Structure

CAS No. 177834-92-3

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Eletriptan HBr Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.
Targets
5-HT1B [1] 5-HT1D [1]
0.92 nM(Ki) 3.14 nM(Ki)
In vitro
In vitro [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan). [1] Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery. [2]
In Vivo
In vivo Eletriptan (<1000 mg/kg, i.v.) produces a dose-dependent reduction of carotid arterial blood flow in the anaesthetised dog. Eletriptan reduces coronary artery diameter with ED50 value of 63 mg/kg in the anaesthetised dog. Eletriptan (<300 mg/kg, i.v.) administered prior to electrical stimulation of the trigeminal ganglion produces a dose-related and complete inhibition of plasma protein extravasation in the dura mater rats. Eletriptan (100 mg/kg, i.v.) produces a complete inhibition of plasma protein extravasation in rat dura mater. [3] Headache response rates are 24% for placebo; 54% for Eletriptan (20 mg);65% for Eletriptan (40 mg);and 77% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Headache-free rates at 2 hours are 6% for placebo, 29% for Eletriptan (40 mg) and 37% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Eletriptan is well tolerated, and the majority of adverse events are mild or moderate in intensity and transient in patients with migraine. [4] Iontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00174395 Completed
Migraine
Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer
 March 2005 Phase 4

Chemical Information & Solubility

Molecular Weight 463.43 Formula

C22H26N2O2S.HBr
CAS No. 177834-92-3 SDF Download Eletriptan HBr SDF
Smiles CN1CCCC1CC2=CNC3=C2C=C(C=C3)CCS(=O)(=O)C4=CC=CC=C4.Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (200.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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