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Open AccessReview

Epibatidine: A Promising Natural Alkaloid in Health

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Student Research Committee, School of Medicine, Bam University of Medical Sciences, Bam 44340847, Iran
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Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
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Interdepartmental Research Centre for Biology and Pathology of Aging, University of Pisa, 55126 Pisa, Italy
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Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo, 5, 35131 Padova (PD), Italy
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Department of Clinical Pharmacy, University of Medicine and Pharmacy Craiova, Craiova 200349, Romania
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Department of Medical Parasitology, Zabol University of Medical Sciences, Zabol 61663-335, Iran
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Department of Pharmaceutical Technology, Avicenna Tajik State Medical University, Rudaki 139, Dushanbe 734003, Tajikistan
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Faculty of Medicine, University of Porto, Alameda Prof. Hernâni Monteiro, 4200-319 Porto, Portugal
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Institute for Research and Innovation in Health (i3S), University of Porto, 4200-135 Porto, Portugal
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Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol 61615-585, Iran
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Department of Chemistry, Richardson College for the Environmental Science Complex, The University of Winnipeg, Winnipeg, MB R3B 2G3, Canada
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Authors to whom correspondence should be addressed.
Biomolecules 2019, 9(1), 6; https://doi.org/10.3390/biom9010006
Received: 20 November 2018 / Revised: 10 December 2018 / Accepted: 17 December 2018 / Published: 23 December 2018
Epibatidine is a natural alkaloid that acts at nicotinic acetylcholine receptors (nAChRs). The present review aims to carefully discuss the affinity of epibatidine and its synthetic derivatives, analogues to nAChRs for α4β2 subtype, pharmacokinetic parameters, and its role in health. Published literature shows a low affinity and lack of binding of epibatidine and its synthetic analogues to plasma proteins, indicating their availability for metabolism. Because of its high toxicity, the therapeutic use of epibatidine is hampered. However, new synthetic analogs endowed from this molecule have been developed, with a better therapeutic window and improved selectivity. All these aspects are also discussed here. On the other hand, many reports are devoted to structure–activity relationships to obtain optically active epibatidine and its analogues, and to access its pharmacological effects. Although pharmacological results are obtained from experimental studies and only a few clinical trials, new perspectives are open for the discovery of new drug therapies. View Full-Text
Keywords: epibatidine; nicotinic acetylcholine receptors; analgesics; ABT-594; ABT-418 epibatidine; nicotinic acetylcholine receptors; analgesics; ABT-594; ABT-418
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Salehi, B.; Sestito, S.; Rapposelli, S.; Peron, G.; Calina, D.; Sharifi-Rad, M.; Sharopov, F.; Martins, N.; Sharifi-Rad, J. Epibatidine: A Promising Natural Alkaloid in Health. Biomolecules 2019, 9, 6.

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