Synthesis of 1-substituted epibatidine analogues and their in vitro and in vivo evaluation as α4β2nicotinic acetylcholine receptor ligands

Thomas S. A. Heugebaert, Melissa Van Overtveldt, Ann De Blieck, Benjamin Wuyts, Patrick Augustijns, Eugenia Ponce-Gámez, Alicia Rivera, Dominic De Groote, Romain A. Lefebvre, Patrick Wouters, Theo Meert, Jacques Devulder, Christian V. Stevens
  • RSC Advances, January 2014, Royal Society of Chemistry
  • DOI: 10.1039/c3ra44379e

In vivo activity of epibatidine analogues

What is it about?

Analogues of epibatidine, a natural compound isolated from the skin of a frog, have been synthesized. The side chain of the natural compound was moved one carbon atom on the azabicyclic skeleton. Although the compounds were active in vitro, the in vivo activity in rats are low due to a low bio-availability.

Why is it important?

The epibatidine analogues prove that the design of the molecules are valuable, however further work needs to be done to improve the bio-availability of the compounds.

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