WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 525179
CAS#: 945493-87-8 (HCl)
Description: GSK 189254A is histamine H3 receptor antagonist for the treatment of narcolepsy. The compound may also be useful in the treatment of dementia and neuropathic pain. Histamine H3 receptor antagonists have been shown to increase the release of neurotransmitters in the brain and to enhance cognition in vivo.
MedKoo Cat#: 525179
Name: GSK 189254 HCl
CAS#: 945493-87-8 (HCl)
Chemical Formula: C21H26ClN3O2
Exact Mass: 351.19468
Molecular Weight: 387.908
Elemental Analysis: C, 65.02; H, 6.76; Cl, 9.14; N, 10.83; O, 8.25
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
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Related CAS #: 945493-87-8 (HCl) 720690-73-3 (free base)
Synonym: GSK 189254A; GSK189254A; GSK-189254A; GSK 189254 HCl; GSK 189254 hydrochloride
IUPAC/Chemical Name: 3-Pyridinecarboxamide, 6-((3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl- hydrochloride
InChi Key: GRQVZNMSXFEEHD-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: O=C(C1=CC=C(OC2=CC=C3CCN(C4CCC4)CCC3=C2)N=C1)NC.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 387.908 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Schou M, Varnäs K, Jureus A, Ahlgren C, Malmquist J, Häggkvist J, Tari L, Wesolowski SS, Throner SR, Brown DG, Nilsson M, Johnström P, Finnema SJ, Nakao R, Amini N, Takano A, Farde L. Discovery and Preclinical Validation of [(11)C]AZ13153556, a Novel Probe for the Histamine Type 3 Receptor. ACS Chem Neurosci. 2016 Feb 17;7(2):177-84. doi: 10.1021/acschemneuro.5b00268. Epub 2015 Nov 30. PubMed PMID: 26529287.
2: Gallezot JD, Planeta B, Nabulsi N, Palumbo D, Li X, Liu J, Rowinski C, Chidsey K, Labaree D, Ropchan J, Lin SF, Sawant-Basak A, McCarthy TJ, Schmidt AW, Huang Y, Carson RE. Determination of receptor occupancy in the presence of mass dose: [11C]GSK189254 PET imaging of histamine H3 receptor occupancy by PF-03654746. J Cereb Blood Flow Metab. 2016 May 20. pii: 0271678X16650697. [Epub ahead of print] PubMed PMID: 27207170.
3: Wang M, Gao M, Steele BL, Glick-Wilson BE, Brown-Proctor C, Shekhar A, Hutchins GD, Zheng QH. A new facile synthetic route to [11C]GSK189254, a selective PET radioligand for imaging of CNS histamine H3 receptor. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4713-8. doi: 10.1016/j.bmcl.2012.05.076. Epub 2012 May 26. PubMed PMID: 22687746.
4: Logan J, Carruthers NI, Letavic MA, Sands S, Jiang X, Shea C, Muench L, Xu Y, Carter P, King P, Fowler JS. Blockade of the brain histamine H3 receptor by JNJ-39220675: preclinical PET studies with [¹¹C]GSK189254 in anesthetized baboon. Psychopharmacology (Berl). 2012 Oct;223(4):447-55. Epub 2012 May 22. PubMed PMID: 22614669; PubMed Central PMCID: PMC3456925.
5: Plisson C, Gunn RN, Cunningham VJ, Bender D, Salinas CA, Medhurst AD, Roberts JC, Laruelle M, Gee AD. 11C-GSK189254: a selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET. J Nucl Med. 2009 Dec;50(12):2064-72. doi: 10.2967/jnumed.109.062919. Epub 2009 Nov 12. PubMed PMID: 19910432.
6: Ashworth S, Rabiner EA, Gunn RN, Plisson C, Wilson AA, Comley RA, Lai RY, Gee AD, Laruelle M, Cunningham VJ. Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET. J Nucl Med. 2010 Jul;51(7):1021-9. doi: 10.2967/jnumed.109.071753. Epub 2010 Jun 16. PubMed PMID: 20554726.
