497963-90-3Relevant academic research and scientific papers
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists
Ahmed, Mahmood,Briggs, Michael A.,Bromidge, Steven M.,Buck, Tania,Campbell, Lorraine,Deeks, Nigel J.,Garner, Ashley,Gordon, Laurie,Hamprecht, Dieter W.,Holland, Vicky,Johnson, Christopher N.,Medhurst, Andrew D.,Mitchell, Darren J.,Moss, Stephen F.,Powles, Jenifer,Seal, Jon T.,Stean, Tania O.,Stemp, Geoffrey,Thompson, Mervyn,Trail, Brenda,Upton, Neil,Winborn, Kim,Witty, David R.
, p. 4867 - 4871 (2007/10/03)
Starting from the potent and selective but poorly brain penetrant 5-HT 6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog.
