Discovery of indole alkaloids with cannabinoid CB1 receptor antagonistic activity

Three indole alkaloids, voacamine ( 1), 3,6-oxidovoacangine ( 2), and a new alkaloid, 5-hydroxy-3,6-oxidovoacangine ( 3), isolated from Voacanga africana were found to exhibit potent cannabinoid CB1 receptor antagonistic activity. This is the first example of CB1 antagonists derived from natural alk...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (7), p.1962-1964
Hauptverfasser:	Kitajima, Mariko, Iwai, Masumi, Kikura-Hanajiri, Ruri, Goda, Yukihiro, Iida, Mitsuru, Yabushita, Hisatoshi, Takayama, Hiromitsu
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonist antagonists Biological and medical sciences Cannabinoid cannabinoids CB1 receptor Drug Discovery General pharmacology Iboga Indole alkaloid indole alkaloids Indole Alkaloids - chemistry Indole Alkaloids - pharmacology Medical sciences Molecular Structure Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Plant Extracts - pharmacology Receptor, Cannabinoid, CB1 - antagonists & inhibitors receptors Spectrometry, Mass, Electrospray Ionization Voacanga Voacanga - chemistry
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Zusammenfassung:	Three indole alkaloids, voacamine ( 1), 3,6-oxidovoacangine ( 2), and a new alkaloid, 5-hydroxy-3,6-oxidovoacangine ( 3), isolated from Voacanga africana were found to exhibit potent cannabinoid CB1 receptor antagonistic activity. This is the first example of CB1 antagonists derived from natural alkaloids.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.02.036