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Histamine Receptors
- Protein Control Ligand
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Quantity Discount Table - Order More To Get More Price Discount
| Quantity | mg | Unit Price ($/mg or $/Unit) | Final Price |
|---|---|---|---|
| 1 | 100 | $16.65 | Total: $1,665.00 |
| 1 | 50 | $19.24 | Total: $962.00 |
| 1 | 25 | $22.57 | Total: $564.25 |
| 1 | 10 | $26.64 | Total: $266.40 |
| 1 | 5 | $31.45 | Total: $157.25 |
Data sheet
| Molecular Formula | C21H26ClN3O2 |
| Molecular Weight | 387.91 |
| CAS Numbers | 720690-73-3 |
| Storage Condition | 0°C (short term), -20°C (long term), desiccated |
| Solubility | DMSO |
| Purity | 98% by HPLC |
More info
A potent and selective H3-receptor inverse agonist developed. It has subnanomolar affinity for the H3 receptor (Ki 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes.
Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs.
Reference
1) Antagonism of supraspinal histamine H3 receptors modulates spinal neuronal activity in neuropathic rats.
McGaraughty S1, Chu KL, Cowart MD, Brioni JD. J Pharmacol Exp Ther. 2012 Oct;343(1):13-20. doi: 10.1124/jpet.112.194761. Epub 2012 Jun 22.
2) Unexpectedly high affinity of a novel histamine H(3) receptor antagonist, GSK239512, in vivo in human brain, determined using PET. Ashworth S1, Berges A, Rabiner EA, Wilson AA, Comley RA, Lai RY, Boardley R, Searle G, Gunn RN, Laruelle M, Cunningham VJ. Br J Pharmacol. 2014 Mar;171(5):1241-9. doi: 10.1111/bph.12505.
3) A new facile synthetic route to [11C]GSK189254, a selective PET radioligand for imaging of CNS histamine H3 receptor.
Wang M1, Gao M, Steele BL, Glick-Wilson BE, Brown-Proctor C, Shekhar A, Hutchins GD, Zheng QH. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4713-8. doi: 10.1016/j.bmcl.2012.05.076. Epub 2012 May 26.
4) Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Wilson DM1, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5.
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