437652-01-2Relevant academic research and scientific papers
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor
Austin, Nigel E,Avenell, Kim Y,Boyfield, Izzy,Branch, Clive L,Hadley, Michael S,Jeffrey, Phillip,Johnson, Christopher N,Macdonald, Gregor J,Nash, David J,Riley, Graham J,Smith, Alexander B,Stemp, Geoffrey,Thewlis, Kevin M,Vong, Antonio K.K,Wood, Martyn D
, p. 685 - 688 (2007/10/03)
Starting from the tetrahydroisoquinoline SB-2770111, a novel series of 5-substituted-2,3-dihydro-1H-isoindoles has been designed. Subsequent optimisation resulted in identification of 19. which has high affinity for the dopamine D3 receptor (pKi 8.3) and ≥ 100-fold selectivity over other aminergic receptors. In rat studies 19 was brain penetrant with an excellent pharmacokinetic profile (oral bioavailability 77%. t1/2 5.2h).
