| Literature DB >> 11266169 |
N E Austin1, K Y Avenell, I Boyfield, C L Branch, M S Hadley, P Jeffrey, C N Johnson, G J Macdonald, D J Nash, G J Riley, A B Smith, G Stemp, K M Thewlis, A K Vong, M D Wood.
Abstract
Starting from the tetrahydroisoquinoline SB-277011 1, 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 > or = 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).Entities:
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Year: 2001 PMID： 11266169 DOI： 10.1016/s0960-894x(01)00037-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823