Chemistry:PHA-543,613
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Short description: Chemical compound
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| Formula | C15H17N3O2 |
| Molar mass | 271.314 g·mol−1 |
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PHA-543,613 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.[1] It reduces excitotoxicity[2] and protects striatal dopaminergic neurons in rat models.[3] It also potentiates cognitive enhancement from memantine,[4][5] decreases dynorphin release[6] and inhibits GSK-B3.[7]
See also
References
- ↑ "Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship". Journal of Medicinal Chemistry 49 (14): 4425–36. July 2006. doi:10.1021/jm0602413. PMID 16821801.
- ↑ "Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an in vivo excitotoxic adult rat model". Neuroscience 356: 52–63. July 2017. doi:10.1016/j.neuroscience.2017.05.019. PMID 28527955. https://zenodo.org/record/1045803.
- ↑ "Assessment of the Protection of Dopaminergic Neurons by an α7 Nicotinic Receptor Agonist, PHA 543613 Using [(18)FLBT-999 in a Parkinson's Disease Rat Model"]. Frontiers in Medicine 2: 61. 2015. doi:10.3389/fmed.2015.00061. PMID 26389120.
- ↑ "Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task". Psychopharmacology 238 (11): 3273–3281. August 2021. doi:10.1007/s00213-021-05942-4. PMID 34387707.
- ↑ "Cognitive Enhancer Effects of Low Memantine Doses Are Facilitated by an Alpha7 Nicotinic Acetylcholine Receptor Agonist in Scopolamine-Induced Amnesia in Rats". Frontiers in Pharmacology 10: 73. 2019. doi:10.3389/fphar.2019.00073. PMID 30804787.
- ↑ "Activation of alpha7 acetylcholine receptors reduces neuropathic pain by decreasing dynorphin A release from microglia". Brain Research 1715: 57–65. July 2019. doi:10.1016/j.brainres.2019.03.016. PMID 30898676.
- ↑ "α7 nicotinic acetylcholine receptor agonism confers neuroprotection through GSK-3β inhibition in a mouse model of intracerebral hemorrhage". Stroke 43 (3): 844–50. March 2012. doi:10.1161/STROKEAHA.111.639989. PMID 22207510.
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