Conessine Explained

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

References

  1. 3445993. 1987. Duez. P. Changes in conessine in stem bark of Holarrhena floribunda in Burkina Faso. Annales pharmaceutiques françaises. 45. 4. 307–13. Chamart. S. Lejoly. J. Hanocq. M. Zeba. B. Sawadogo. M. Guissou. P. Molle. L.
  2. 17541193. 2007. Kumar. N. Steroidal alkaloids from Holarrhena antidysenterica (L.) WALL. Chemical & Pharmaceutical Bulletin. 55. 6. 912–4. Singh. B. Bhandari. P. Gupta. A. P.. Kaul. V. K.. 10.1248/cpb.55.912. free.
  3. 15863333. 2005. Zirihi. G. N.. Isolation, characterization and antiplasmodial activity of steroidal alkaloids from Funtumia elastica (Preuss) Stapf. Bioorganic & Medicinal Chemistry Letters. 15. 10. 2637–40. Grellier. P. Guédé-Guina. F. Bodo. B. Mambu. L. 10.1016/j.bmcl.2005.03.021.
  4. 18194865. 2008. Santora. V. J.. A new family of H3 receptor antagonists based on the natural product Conessine. Bioorganic & Medicinal Chemistry Letters. 18. 4. 1490–4. Covel. J. A.. Hayashi. R. Hofilena. B. J.. Ibarra. J. B.. Pulley. M. D.. Weinhouse. M. I.. Sengupta. D. Duffield. J. J.. Semple. G. Webb. R. R.. Sage. C. Ren. A. Pereira. G. Knudsen. J. Edwards. J. E.. Suarez. M. Frazer. J. Thomsen. W. Hauser. E. Whelan. K. Grottick. A. J.. 10.1016/j.bmcl.2007.12.059.
  5. 10.1021/jm8003625. 18683917. The Alkaloid Conessine and Analogues as Potent Histamine H3Receptor Antagonists. Journal of Medicinal Chemistry. 51. 17. 5423–30. 2008. Zhao. Chen. Sun. Minghua. Bennani. Youssef L.. Gopalakrishnan. Sujatha M.. Witte. David G.. Miller. Thomas R.. Krueger. Kathleen M.. Browman. Kaitlin E.. Thiffault. Christine. Wetter. Jill. Marsh. Kennan C.. Hancock. Arthur A.. Esbenshade. Timothy A.. Cowart. Marlon D..

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Conessine".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.