Chemistry:Huprine X
From HandWiki
Short description: Chemical compound
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| Formula | C18H19ClN2 |
| Molar mass | 298.81 g·mol−1 |
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Huprine X is a synthetic cholinergic compound developed as a hybrid between the natural product Huperzine A and the synthetic drug tacrine. It is one of the most potent reversible inhibitors of acetylcholinesterase known, with a binding affinity of 0.026nM,[1] as well as showing direct agonist activity at both nicotinic and muscarinic acetylcholine receptors.[2][3] In animal studies it has nootropic and neuroprotective effects, and is used in research into Alzheimer's disease,[4][5][6][7] and although huprine X itself has not been researched for medical use in humans, a large family of related derivatives have been developed.[8][9][10]
References
- ↑ "Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer's disease". Molecular Pharmacology 57 (2): 409–17. February 2000. PMID 10648652.
- ↑ "Interaction of a new potent anticholinesterasic compound (+/-)huprine X with muscarinic receptors in rat brain". Neuroscience Letters 325 (2): 103–6. June 2002. doi:10.1016/s0304-3940(02)00245-8. PMID 12044632.
- ↑ "Potentiation effects of (+/-)huprine X, a new acetylcholinesterase inhibitor, on nicotinic receptors in rat cortical synaptosomes". Neuropharmacology 46 (1): 95–102. January 2004. doi:10.1016/j.neuropharm.2003.08.005. PMID 14654101.
- ↑ "Behavioural effects and regulation of PKCalpha and MAPK by huprine X in middle aged mice". Pharmacology, Biochemistry, and Behavior 95 (4): 485–93. June 2010. doi:10.1016/j.pbb.2010.03.013. PMID 20363245.
- ↑ "Huprine X and huperzine A improve cognition and regulate some neurochemical processes related with Alzheimer's disease in triple transgenic mice (3xTg-AD)". Neuro-Degenerative Diseases 11 (3): 129–40. 2013. doi:10.1159/000336427. PMID 22626981.
- ↑ "Behavioural effects of novel multitarget anticholinesterasic derivatives in Alzheimer's disease". Behavioural Pharmacology 28 (2 and 3-Spec Issue): 124–131. April 2017. doi:10.1097/FBP.0000000000000292. PMID 28125507.
- ↑ "Huprine X Attenuates The Neurotoxicity Induced by Kainic Acid, Especially Brain Inflammation". Basic & Clinical Pharmacology & Toxicology 122 (1): 94–103. January 2018. doi:10.1111/bcpt.12852. PMID 28724203.
- ↑ "Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors". Bioorganic & Medicinal Chemistry 17 (13): 4523–36. July 2009. doi:10.1016/j.bmc.2009.05.005. PMID 19473849.
- ↑ "New huprine derivatives functionalized at position 9 as highly potent acetylcholinesterase inhibitors". ChemMedChem 6 (5): 876–88. May 2011. doi:10.1002/cmdc.201000523. PMID 21344648.
- ↑ "Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases". Journal of Medicinal Chemistry 55 (2): 661–9. January 2012. doi:10.1021/jm200840c. PMID 22185619.
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