General
Preferred name
ELETRIPTAN
Synonyms
ELETRIPTAN HYDROBROMIDE ()
UK-116044 ()
Eletriptan HBr ()
[3H]eletriptan ()
Eletriptan (hydrobromide) ()
UK-116044 (hydrobromide) ()
UK-116044-04 ()
NSC-759258 ()
UK-116,044-04 ()
Relpax ()
UK-116,044 ()
UK-116044-04 FREE BASE ()
UK-116,044-04 [AS HYDROBROMIDE) ()
UK-116,044-04 FREE BASE ()
[3H]eletriptan ()
P&D ID
PD010168
CAS
177834-92-3
143322-58-1
Tags
available
drug candidate
drug
Approved by
FDA
First approval
2002
Drug Status
investigational
approved
Drug indication
Migraine
Discovery agent
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. In contrast, eletriptan displays insignificant pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. While the full mechanism of action of 5-HT receptor agonists in relieving migrains is not fully elucidated, it is proposed that the activation of 5-HT1 receptors located on intracranial blood vessels leads to vasoconstriction that correlates with the relief of migraine headaches. It is also proposed that the activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system leads to the inhibition of release of pro-inflammatory neuropeptides.
DESCRIPTION Approved as eletriptan hydrobromide. (GtoPdb)
DESCRIPTION Orally active, selective 5-HT1B/1D agonist (Tocriscreen Plus)
DESCRIPTION Orally active, selective 5-HT1B/1D agonist (Tocriscreen Total)
Compound Sets
28
AdooQ Bioactive Compound Library
A11418
Axon Medchem Screening Library
2050
Cayman Chemical Bioactives
20048
ChEMBL Approved Drugs
CHEMBL1201003
CHEMBL1510
ChEMBL Drugs
CHEMBL1201003
CHEMBL1510
Concise Guide to Pharmacology 2017/18
40
118
Concise Guide to Pharmacology 2019/20
40
118
Concise Guide to Pharmacology 2021/22
40
118
Concise Guide to Pharmacology 2023/24
40
118
Drug Repurposing Hub
DrugBank
DB00216
DrugBank Approved Drugs
DB00216
DrugCentral
995
DrugCentral Approved Drugs
995
DrugMAP
DMW649X
DMDTYRV
DrugMAP Approved Drugs
DMW649X
EU-OPENSCREEN Bioactive Compound Library
EOS101352
Guide to Pharmacology
40
118
MedChem Express Bioactive Compound Library
HY-A0010
NCATS Inxight Approved Drugs
22QOO9B8KI
NPC Screening Collection
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
eletriptan-hydrobromide
TargetMol Bioactive Compound Library
T0216
The Spectrum Collection
Tocriscreen Plus
3862
Tocriscreen Total
External IDs
63
Properties
(calculated by RDKit )
Molecular Weight
382.17
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
3.82
TPSA
53.17
Fraction CSP3
0.36
Chiral centers
1.0
Largest ring
6.0
QED
0.71
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Target
5-HT1B
5-HT1D
HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2B, HTR7
5-HT1B/1D agonist
5-HT Receptor
Indication
migraine headache
MOA
serotonin receptor agonist
Therapeutic Class
Antimigraine Agents
Source data