1048964-46-0Relevant academic research and scientific papers
Novel H3 receptor antagonists with improved pharmacokinetic profiles
Santora, Vincent J.,Covel, Jonathan A.,Hayashi, Rena,Hofilena, Brian J.,Ibarra, Jason B.,Pulley, Michelle D.,Weinhouse, Michael I.,Semple, Graeme,Ren, Albert,Pereira, Guilherme,Edwards, Jeffrey E.,Suarez, Marissa,Frazer, John,Thomsen, William,Hauser, Erin,Lorea, Jodie,Grottick, Andrew J.
scheme or table, p. 4133 - 4136 (2009/05/30)
A new series of H3 antagonists derived from the natural product Conessine are presented. Several compounds from these new series retain the potency and selectivity of earlier diamine based analogs while exhibiting improved PK characteristics. O
A new family of H3 receptor antagonists based on the natural product Conessine
Santora, Vincent J.,Covel, Jonathan A.,Hayashi, Rena,Hofilena, Brian J.,Ibarra, Jason B.,Pulley, Michelle D.,Weinhouse, Michael I.,Sengupta, Dipanjan,Duffield, Jonathan J.,Semple, Graeme,Webb, Robert R.,Sage, Carleton,Ren, Albert,Pereira, Guilherme,Knudsen, Jens,Edwards, Jeffrey E.,Suarez, Marissa,Frazer, John,Thomsen, William,Hauser, Erin,Whelan, Kevin,Grottick, Andrew J.
, p. 1490 - 1494 (2008/12/21)
A new family of Histamine H3 receptor antagonists (5a-t) has been prepared based on the structure of the natural product Conessine, a known H3 antagonist. Several members of the new series are highly potent and selective binders of rat and human H3 receptors and display inverse agonism at the human H3 receptor. Compound 5n exhibited promising rat pharmacokinetic properties and demonstrated functional antagonism of the H3 receptor in an in-vivo pharmacological model.
