Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo.

@article{Briggs1997FunctionalCO,
  title={Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo.},
  author={Clark Briggs and David J. Anderson and Jorge D. Brioni and Jerry J. Buccafusco and Michael J. Buckley and Jeffrey E. Campbell and Michael W. Decker and D L Donnelly-roberts and Richard L. Elliott and Murali M Gopalakrishnan and Mark W. Holladay and Yu Hua Hui and William J. Jackson and Dai Jin Kim and Kennan C. Marsh and Andrea O'Neill and Mark A. Prendergast and Keith B Ryther and James P. Sullivan and Stephen Arneric},
  journal={Pharmacology, biochemistry, and behavior},
  year={1997},
  volume={57 1-2},
  pages={231-41}
}
(2.4)-Dimethoxybenzylidene anabaseine dihydrochloride (GTS-21), a compound that interacts with rat neuronal nicotinic acetylcholine receptors (nAChRs), was evaluated using human recombinant nAChRs in vitro and various pharmacokinetic and behavioral models in rodents, dogs and monkeys. GTS-21 bound to human alpha 4 beta 2 nAChR (K1-20 nM) 100-fold more potently than to human alpha 7 nAChR, and was 18- and 2-fold less potent than (-)-nicotine at human alpha 4 beta 2 and alpha 7 nAChR… CONTINUE READING