Title of article
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor
Author/Authors
Nigel E. Austin، نويسنده , , Kim Y. Avenell، نويسنده , , Izzy Boyfield، نويسنده , , Clive L. Branch، نويسنده , , Michael S. Hadley، نويسنده , , Phillip Jeffrey، نويسنده , , Christopher N. Johnson، نويسنده , , Gregor J. Macdonald، نويسنده , , David J. Nash، نويسنده , , Graham J. Riley، نويسنده , , Alexander B. Smith، نويسنده , , Geoffrey Stemp، نويسنده , , Kevin M. Thewlis، نويسنده , , Antonio K. K. Vong، نويسنده , , Martyn D. Wood، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
4
From page
685
To page
688
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 ≥100-fold selectivity over other aminergic receptors. In rat studies 19 was brain penetrant with an excellent pharmacokinetic profile (oral bioavailability 77%, t1/2 5.2 h).
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791251
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