GSK 189254 HCl
| Code | Size | Price |
|---|
| TAR-T19628-5mg | 5mg | £850.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T19628-50mg | 50mg | £1,661.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T19628-100mg | 100mg | £2,079.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
GSK 189254A is a histamine H3 receptor antagonist for the treatment of narcolepsy. Histamine H3 receptor antagonists have been shown to increase the release of neurotransmitters in the brain and to enhance cognition in vivo. The compound may also be useful in the treatment of dementia and neuropathic pain.
CAS:
945493-87-8
Formula:
C21H26ClN3O2
Molecular Weight:
387.91
Purity:
0.98
SMILES:
Cl.CNC(=O)c1ccc(Oc2ccc3CCN(CCc3c2)C2CCC2)nc1
References
1. Schou M, Varn?s K, Jureus A, Ahlgren C, Malmquist J, H?ggkvist J, Tari L, Wesolowski SS, Throner SR, Brown DG, Nilsson M, Johnstr?m 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 [??C]GSK189254 in anesthetized baboon. Psychopharmacology (Berl). 2012 Oct;223(4):447-55. Epub 2012 May 22. PubMed PMID: 22614669; PubMed Central PMCID: PMC3456925.