Drug General Information
Drug ID
D06FKC
Former ID
DIB006653
Drug Name
Eltoprazine
Synonyms
Piperazine derivative (ADHD), PsychoGenics/ReqMed Company; 5-HT1A/5-HT1B agonist and 5-HT2C antagonist (ADHD), PsychoGenics/ReqMed Company
Drug Type
Small molecular drug
Indication Aggressive non-hodgkin's lymphoma [ICD9: 200, 201, 202, 202.8, 208.9; ICD10:C81, C81-C86, C82-C85, C91-C95] Phase 2 [523309]
Company
Amarantus bioscience; psychogenics
Structure
Download
2D MOL

3D MOL

Formula
C12H16N2O2
Canonical SMILES
C1CN(CCN1)c2cccc3OCCOc23
InChI
1S/C12H16N2O2/c1-2-10(14-6-4-13-5-7-14)12-11(3-1)15-8-9-16-12/h1-3,13H,4-9H2
InChIKey
WVLHGCRWEHCIOT-UHFFFAOYSA-N
CAS Number
CAS 98224-03-4
PubChem Compound ID
Target and Pathway
Target(s) 5-hydroxytryptamine 1A receptor Target Info Agonist [551057]
5-hydroxytryptamine 2C receptor Target Info Antagonist [551057]
5-hydroxytryptamine 1B receptor Target Info Agonist [551057], [551730]
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Serotonergic synapsehsa04020:Calcium signaling pathway
Gap junction
Serotonergic synapse
Inflammatory mediator regulation of TRP channelshsa04024:cAMP signaling pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
5HT1 type receptor mediated signaling pathwayP04374:5HT2 type receptor mediated signaling pathwayP00026:Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
5HT1 type receptor mediated signaling pathway
Reactome Serotonin receptors
G alpha (i) signalling eventsR-HSA-390666:Serotonin receptors
G alpha (q) signalling eventsR-HSA-390666:Serotonin receptors
G alpha (i) signalling events
WikiPathways Serotonin HTR1 Group and FOS Pathway
SIDS Susceptibility Pathways
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signalingWP732:Serotonin Receptor 2 and ELK-SRF/GATA4 signaling
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR downstream signalingWP722:Serotonin HTR1 Group and FOS Pathway
GPCR downstream signaling
References
Ref 523309ClinicalTrials.gov (NCT01266174) Effects of Eltoprazine on Cognitive Impairment Associated With Schizophrenia (CIAS) in Adults. U.S. National Institutes of Health.
Ref 551057Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
Ref 551730Sustained pain relief with dihydroergotamine in migraine is potentially due to persistent binding to 5-HT1B and 5-HT1D receptors. . The Journal of Headache and Pain 201314(Suppl 1):P75.

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