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Conessine

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Conessine is a steroid alkaloid found in a number of plant species from the Apocynaceae family, including Holarrhena floribunda,[1] Holarrhena antidysenterica[2] and Funtumia elastica,[3] several of which are used in traditional herbal medicine as a treatment for amoebic dysentery.[4] It acts as a histamine antagonist, selective for the H3 subtype (with an affinity of pKi=8.27; Ki~5nM).[5] It was also found to have long CNS clearance times, high blood-brain barrier penetration and high affinity for the adrenergic receptors.[6]

References

  1. Duez P, Chamart S, Lejoly J, Hanocq M, Zeba B, Sawadogo M, Guissou P, Molle L. Changes in conessine in stem bark of Holarrhena floribunda in Burkina Faso. Annales Pharmaceutiques Francaises (French). 1987;45(4):307-13. PMID 3445993
  2. Kumar N, Singh B, Bhandari P, Gupta AP, Kaul VK. Steroidal alkaloids from Holarrhena antidysenterica (L.) WALL. Chemical and Pharmaceutical Bulletin (Tokyo). 2007 Jun;55(6):912-4. PMID 17541193
  3. Zirihi GN, Grellier P, Guédé-Guina F, Bodo B, Mambu L. Isolation, characterization and antiplasmodial activity of steroidal alkaloids from Funtumia elastica (Preuss) Stapf. Bioorganic and Medicinal Chemistry Letters. 2005 May 16;15(10):2637-40. PMID 15863333
  4. Garg S, Bhutani KK. Chromatographic analysis of Kutajarista--an ayurvedic polyherbal formulation. Phytochemical Analysis. 2008 Jul;19(4):323-8. PMID 18197597
  5. Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Sengupta D, Duffield JJ, Semple G, Webb RR, Sage C, Ren A, Pereira G, Knudsen J, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Whelan K, Grottick AJ. A new family of H3 receptor antagonists based on the natural product Conessine. Bioorganic and Medicinal Chemistry Letters. 2008 Feb 15;18(4):1490-4. PMID 18194865
  6. Chen Zhao, Minghua Sun, Youssef L. Bennani, Sujatha M. Gopalakrishnan, David G. Witte, Thomas R. Miller, Kathleen M. Krueger, Kaitlin E. Browman, Christine Thiffault, Jill Wetter, Kennan C. Marsh, Arthur A. Hancock, Timothy A. Esbenshade, Marlon D. Cowart, 'The Alkaloid Conessine and Analogues as Potent Histamine H3 Receptor Antagonists', Journal of Medicinal Chemistry, 51/17 (2008), 5423-5430.
 

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