Chemistry:Ispronicline
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| Formula | C14H22N2O |
| Molar mass | 234.343 g·mol−1 |
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Ispronicline (TC-1734, AZD-3480) is an experimental drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease, but is no longer under development.[1]
It has also progressed to phase II as a potential treatment for ADHD. With dosages of 50 mg/day showing a significant improvement in ADHD symptoms[2][3]
Ispronicline is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects.
Early stage clinical trials showed that ispronicline was well tolerated, with the main side effects being dizziness and headache.[4][5][6][7][8] However, mid-stage clinical trials failed to show sufficient efficacy to continue development as a pharmaceutical drug.[1]
See also
References
- ↑ 1.0 1.1 "Targacept Drops Development of Alzheimer's Drug". Wall Street Journal. 14 July 2014. https://www.wsj.com/articles/targacept-drops-development-of-alzheimers-drug-1405367773.
- ↑ "AZD3480, a novel nicotinic receptor agonist, for the treatment of attention-deficit/hyperactivity disorder in adults". Biological Psychiatry 75 (3): 207–214. February 2014. doi:10.1016/j.biopsych.2013.06.002. PMID 23856296.
- ↑ AstraZeneca (2009-10-29). "An Exploratory Trial of AZD3480 (TC-1734) for the Treatment of Adult Attention-Deficit/Hyperactivity Disorder (ADHD)". https://clinicaltrials.gov/ct2/show/study/NCT00683462.
- ↑ "TC-1734: an orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects". CNS Drug Reviews 10 (2): 147–166. 2004. doi:10.1111/j.1527-3458.2004.tb00010.x. PMID 15179444.
- ↑ "Pharmacokinetics and safety profile of ispronicline (TC-1734), a new brain nicotinic receptor partial agonist, in young healthy male volunteers". Journal of Clinical Pharmacology 46 (7): 715–726. July 2006. doi:10.1177/0091270006288730. PMID 16809797.
- ↑ "Ispronicline: a novel alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties". Journal of Molecular Neuroscience 30 (1–2): 19–20. 2006. doi:10.1385/JMN:30:1:19. PMID 17192610.
- ↑ "Effects of TC-1734 (AZD3480), a selective neuronal nicotinic receptor agonist, on cognitive performance and the EEG of young healthy male volunteers". Psychopharmacology 191 (4): 919–929. May 2007. doi:10.1007/s00213-006-0675-x. PMID 17225162.
- ↑ "Effect of ispronicline, a neuronal nicotinic acetylcholine receptor partial agonist, in subjects with age associated memory impairment (AAMI)". Journal of Psychopharmacology 21 (2): 171–178. March 2007. doi:10.1177/0269881107066855. PMID 17329297.
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