GSK-189254A

Investigational

CNC(=O)C1=CC=C(OC2=CC=C3CCN(CCC3=C2)C4CCC4)N=C1

InChIKey=WROHEWWOCPRMIA-UHFFFAOYSA-N

InChI=1S/C21H25N3O2/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)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H3 receptor 44 Target ID: CHEMBL264 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17327487	Antagonist 2778		9.6 null [pKi]

PubMed

Title	Date	PubMed
Soraprazan: setting new standards in inhibition of gastric acid secretion.	2007 Jun	17369284
Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.	2009 May	19413575
Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over-expressing TASTPM mice.	2009 May	19222483
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 Jan	19815811
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 Jul 14	21634396

Patents

Substance Class	Chemical Created by `admin` on `Sat Dec 16 07:01:28 GMT 2023` Edited by `admin` on `Sat Dec 16 07:01:28 GMT 2023`
Record UNII	5T4TX6CO53
Record Status	`Validated (UNII)`
Record Version

Name

Type

Language

GSK-189254A

Common Name

English

GSK-189254 FREE BASE

Code

English

6-((3-CYCLOBUTYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPIN-7-YL)OXY)-N-METHYL-3-PYRIDINECARBOXAMIDE

Systematic Name

English

GSK-189254

Code

English

Code System Code Type Description

SMS_ID

300000042429