ChemicalBook > CAS DataBase List > GSK 189254A

GSK 189254A

Description References

Product Name: GSK 189254A
CAS No.: 720690-73-3
Chemical Name: GSK 189254A
Synonyms: CS-2905;GSK 189254A;GSK189254A, 10 mM in DMSO;histamine H3 receptor antagonist GS189254A;Histamine Receptor,GSK-189254,GSK 189254,GSK-189254A,inhibit,GSK189254A,Inhibitor;6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-MethylnicotinaMide;N-(4-METHOXYBENZYL)-1-[(4-METHYLPHENYL)SULFONYL]-1H-PYRROLO[2,3-B]PYRIDIN-4-AMINE;6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methylpyridine-3-carboxamide;3-Pyridinecarboxamide, 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-
CBNumber: CB52627923
Molecular Formula: C21H25N3O2
Formula Weight: 351.44
MOL File: 720690-73-3.mol

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GSK 189254A Property

Boiling point:: 545.0±50.0 °C(Predicted)
Density: 1.195±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:25.0(Max Conc. mg/mL);71.13(Max Conc. mM)
form: A solid
pka: 14.26±0.46(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene

Product number: CS-6206
Product name: GSK189254A
Purity: 98.45%
Packaging: 1mg
Price: $60
Updated: 2021/12/16

ChemScene

Product number: CS-6206
Product name: GSK189254A
Purity: 98.45%
Packaging: 5mg
Price: $100
Updated: 2021/12/16

ChemScene

Product number: CS-6206
Product name: GSK189254A
Purity: 98.45%
Packaging: 10mg
Price: $150
Updated: 2021/12/16

ChemScene

Product number: CS-6206
Product name: GSK189254A
Purity: 98.45%
Packaging: 50mg
Price: $450
Updated: 2021/12/16

ChemScene

Product number: CS-6206
Product name: GSK189254A
Purity: 98.45%
Packaging: 100mg
Price: $650
Updated: 2021/12/16

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GSK 189254A Chemical Properties,Usage,Production

Description

GSK189254A is a histamine H3 receptor antagonist for the treatment of narcolepsy.It may also be useful for the treatment of dementia and neuropathic pain. Its pharmacological effect may be related to its effect on increasing the release neurotransmitter in the brain. Microdialysis studies demonstrated that GSK189254 increased the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254 significantly improved performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift. These data suggest that GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer's disease and other cognitive disorders.

References

Medhurst, Andrew D., and A. I. J. Beresford. "GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models." Alzheimers & Dementia 321.3(2007):1032.
Plisson, Christophe, et al. "PET imaging of the CNS histamine H3 receptor using [11C] GSK189254A." Neuroimage 31.1(2006):T47-T47.
http://medkoo.com/products/10117

Uses

GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

in vivo

GSK189254 (0.3-3 mg/kg p.o.) increases the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254 significantly improves performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift^[1]. In Ox+/+ and Ox?/? mice, acute administration of GSK189254 increases W and decreases slow wave and paradoxical sleep to a similar degree to modafinil, while it reduces narcoleptic episodes in Ox?/? mice^[2].

IC 50

H₃ receptor

References

[1] Medhurst AD, et al. GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. DOI:10.1124/jpet.107.120311
[2] Guo RX, et al. Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.Br J Pharmacol. 2009 May;157(1):104-17. DOI:10.1111/j.1476-5381.2009.00205.x

GSK 189254A Preparation Products And Raw materials

Raw materials

Preparation Products

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720690-73-3, GSK 189254ARelated Search:

daprodustat N-((S)-1-(4-((S)-2-(2,4-dichlorophenylsulfonaMido)-3-hydroxypropanoyl)piperazin-1-yl)-4-Methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxaMide GSK-2126458 ABT 702 Dihydrochloride Danirixin GSK1940029 GSK2110183 gsk2200150a 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide 4-Methoxy-N-(2,4,6-triMethylphenyl)benzenesulfonaMide, 97%

GSK 189254A

6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-MethylnicotinaMide

N-(4-METHOXYBENZYL)-1-[(4-METHYLPHENYL)SULFONYL]-1H-PYRROLO[2,3-B<WBR />]PYRIDIN-4-AMINE

6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methylpyridine-3-carboxamide

histamine H3 receptor antagonist GS189254A

CS-2905

3-Pyridinecarboxamide, 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-

Histamine Receptor,GSK-189254,GSK 189254,GSK-189254A,inhibit,GSK189254A,Inhibitor

GSK189254A, 10 mM in DMSO

720690-73-3