Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H25N3O2.ClH |
| Molecular Weight | 387.903 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CNC(=O)C1=CC=C(OC2=CC=C3CCN(CCC3=C2)C4CCC4)N=C1
InChI
InChIKey=GRQVZNMSXFEEHD-UHFFFAOYSA-N
InChI=1S/C21H25N3O2.ClH/c1-22-21(25)17-6-8-20(23-14-17)26-19-7-5-15-9-11-24(18-3-2-4-18)12-10-16(15)13-19;/h5-8,13-14,18H,2-4,9-12H2,1H3,(H,22,25);1H
| Molecular Formula | C21H25N3O2 |
| Molecular Weight | 351.4421 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL264 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17327487 |
9.6 null [pKi] |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. | 2011-07-14 |
|
| Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems. | 2010-10-01 |
|
| When reversible ligands do not reverse, and other modelers' dilemmas. | 2010-07 |
|
| Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET. | 2010-07 |
|
| Regional differential effects of the novel histamine H3 receptor antagonist 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254) on histamine release in the central nervous system of freely moving rats. | 2010-01 |
|
| 11C-GSK189254: a selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET. | 2009-12 |
|
| H3 receptor antagonism enhances NCAM PSA-mediated plasticity and improves memory consolidation in odor discrimination and delayed match-to-position paradigms. | 2009-11 |
|
| Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice. | 2009-05 |
|
| Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over-expressing TASTPM mice. | 2009-05 |
|
| Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain. | 2008-08-15 |
|
| Soraprazan: setting new standards in inhibition of gastric acid secretion. | 2007-06 |
|
| GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. | 2007-06 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:46:31 GMT 2025
by
admin
on
Mon Mar 31 21:46:31 GMT 2025
|
| Record UNII |
4AJV79N1A6
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| Record Status |
Validated (UNII)
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| Record Version |
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Created by
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945493-87-8
Created by
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4AJV79N1A6
Created by
admin on Mon Mar 31 21:46:31 GMT 2025 , Edited by admin on Mon Mar 31 21:46:31 GMT 2025
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