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.[medical citation needed]
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
- ^ a b Armental M (14 July 2014). "Targacept Drops Development of Alzheimer's Drug". Wall Street Journal.
- ^ Potter AS, Dunbar G, Mazzulla E, Hosford D, Newhouse PA (February 2014). "AZD3480, a novel nicotinic receptor agonist, for the treatment of attention-deficit/hyperactivity disorder in adults". Biological Psychiatry. 75 (3): 207–214. doi:10.1016/j.biopsych.2013.06.002. PMID 23856296. S2CID 44717647.
- ^ AstraZeneca (2009-10-29). "An Exploratory Trial of AZD3480 (TC-1734) for the Treatment of Adult Attention-Deficit/Hyperactivity Disorder (ADHD)". Targacept Inc.
- ^ Gatto GJ, Bohme GA, Caldwell WS, Letchworth SR, Traina VM, Obinu MC, et al. (2004). "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. doi:10.1111/j.1527-3458.2004.tb00010.x. PMC 6741718. PMID 15179444.
- ^ Dunbar G, Demazières A, Monreal A, Cisterni C, Metzger D, Kuchibhatla R, et al. (July 2006). "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. doi:10.1177/0091270006288730. PMID 16809797. S2CID 22499622.
- ^ Lippiello P, Letchworth SR, Gatto GJ, Traina VM, Bencherif M (2006). "Ispronicline: a novel alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties". Journal of Molecular Neuroscience. 30 (1–2): 19–20. doi:10.1385/JMN:30:1:19. PMID 17192610. S2CID 195688187.
- ^ Dunbar G, Boeijinga PH, Demazières A, Cisterni C, Kuchibhatla R, Wesnes K, et al. (May 2007). "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. doi:10.1007/s00213-006-0675-x. PMID 17225162. S2CID 10920515.
- ^ Dunbar GC, Inglis F, Kuchibhatla R, Sharma T, Tomlinson M, Wamsley J (March 2007). "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. doi:10.1177/0269881107066855. PMID 17329297. S2CID 10056476.