coronaridine

Coronaridine congers are important in drug discovery and development due to multiple actions on different targets. They have ability to inhibit Ca_v2.2 channel,{{cite journal |vauthors=Arias HR, Tae HS, Micheli L, Yousuf A, Ghelardini C, Adams DJ, Di Cesare Mannelli L |title=Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2.2 channels |journal=Neuropharmacology |volume=175 |issue= |article-number=108194 |date=September 2020 |pmid=32540451 |doi=10.1016/j.neuropharm.2020.108194 |url= |issn=|hdl=2158/1213504 |s2cid=219705597 |hdl-access=free }} modulate and inhibit subunits of nAChr selectively such as α9α10,{{cite journal |vauthors=Arias HR, Tae HS, Micheli L, Yousuf A, Ghelardini C, Adams DJ, Di Cesare Mannelli L |title=Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2.2 channels |journal=Neuropharmacology |volume=175 |issue= |article-number=108194 |date=September 2020 |pmid=32540451 |doi=10.1016/j.neuropharm.2020.108194 |url= |issn=|hdl=2158/1213504 |s2cid=219705597 |hdl-access=free }} α3β4{{cite journal |vauthors=Arias HR, Targowska-Duda KM, Feuerbach D, Jozwiak K |title=Coronaridine congeners inhibit human α3β4 nicotinic acetylcholine receptors by interacting with luminal and non-luminal sites |journal=The International Journal of Biochemistry & Cell Biology |volume=65 |issue= |pages=81–90 |date=August 2015 |pmid=26022277 |doi=10.1016/j.biocel.2015.05.015 |url= |issn=|doi-access=free }}{{cite journal |vauthors=Arias HR, Lykhmus O, Uspenska K, Skok M |title=Coronaridine congeners modulate mitochondrial α3β4* nicotinic acetylcholine receptors with different potency and through distinct intra-mitochondrial pathways |journal=Neurochemistry International |volume=114 |issue= |pages=26–32 |date=March 2018 |pmid=29277577 |doi=10.1016/j.neuint.2017.12.008 |s2cid=3675707 |url= |issn=}} and potentiate GABA_A activity.{{cite journal |vauthors=Arias HR, Do Rego JL, Do Rego JC, Chen Z, Anouar Y, Scholze P, Gonzales EB, Huang R, Chagraoui A |title=Coronaridine congeners potentiate GABAA receptors and induce sedative activity in mice in a benzodiazepine-insensitive manner |journal=Progress in Neuro-psychopharmacology & Biological Psychiatry |volume=101 |issue= |article-number=109930 |date=July 2020 |pmid=32194202 |doi=10.1016/j.pnpbp.2020.109930 |s2cid=212734631 |url= https://hal.archives-ouvertes.fr/hal-03489760/file/S027858461931019X.pdf|issn=}}

Coronaridine has been reported to bind to an assortment of molecular sites, including: μ-opioid (K_i = 2.0 μM), δ-opioid (K_i = 8.1 μM), and κ-opioid receptors (K_i = 4.3 μM), NMDA receptor (K_i = 6.24 μM) (as an antagonist),{{cite book| vauthors = Wiart C |title=Lead Compounds from Medicinal Plants for the Treatment of Neurodegenerative Diseases|url=https://books.google.com/books?id=o3opAgAAQBAJ&pg=PA67|date=16 December 2013|publisher=Academic Press|isbn=978-0-12-398383-1|pages=67–69, 73}} and nAChRs (as an antagonist).{{cite book| vauthors = Polya G |title=Biochemical Targets of Plant Bioactive Compounds: A Pharmacological Reference Guide to Sites of Action and Biological Effects|url=https://books.google.com/books?id=Q20_AJ3wQOoC&pg=PA203|date=15 May 2003|publisher=CRC Press|isbn=978-0-203-01371-7|pages=203–}} It has also been found to inhibit the enzyme acetylcholinesterase, act as a voltage-gated sodium channel blocker,{{cite book | vauthors = Popik P, Skolnick P | chapter = Pharmacology of Ibogaine and Ibogaine-Related Alkaloids | veditors = Cordell GA |title=The Alkaloids. Chemistry and Biology | volume = 52 |date=1999 |publisher=Academic Press |location=San Diego |isbn=978-0-08-086576-8 |pages=197–232 (222) | chapter-url = https://books.google.com/books?id=bE503LRsawYC&pg=PA22}} and displays estrogenic activity in rodents. In contrast to ibogaine and other iboga alkaloids, coronaridine does not bind to either the σ₁ or σ₂ receptor.

• Dregamine
• Ibogaine
• Ibogamine
• Tabernanthine
• Voacangine

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Category:Acetylcholinesterase inhibitors

Category:Alkaloids

Category:Alkaloids found in Iboga

Category:Carboxylate esters

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Category:Nicotinic antagonists

Category:NMDA receptor antagonists

Category:Opioids

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Category:Sodium channel blockers