A novel series of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 15, 1997, Pages 1995-1998

  Boyfield, Izzy ^a   Coldwell, Martyn C ^a   Hadley, Michael S ^a   Johnson, Christopher N ^a   Riley, Graham J ^a   Scott, Emma E ^a   Stacey, Rachel ^a   Stemp, Geoffrey ^a   Thewlis, Kevin M ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 [N [4 (4 PHENYLBENZAMIDO)BUTYL] N PROPYLAMINO] 5 TRIFLUOROMETHANESULFONYLOXYTETRALIN; 2 AMINOTETRALIN DERIVATIVE; 5 CYCLOPROPYLMETHOXY 2 [N [4 (4 PHENYLBENZAMIDO)BUTYL] N PROPYLAMINO]TETRALIN; 5 METHANESULFONYLOXY 2 [N [4 (4 PHENYLBENZAMIDO0BUTYL] N PROPYL]TETRALIN; ADENYLATE CYCLASE; DOPAMINE 3 RECEPTOR; DOPAMINE 3 RECEPTOR BLOCKING AGENT; DOPAMINE RECEPTOR; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CHO CELL; CONTROLLED STUDY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; IN VITRO STUDY; NONHUMAN; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION;

EID: 0030802322     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00350-8     Document Type: Article

References (11)

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9. For details of the microphysiometer method see Boyfield, I.; Brown, T.H.; Coldwell, M.C.; Cooper, D.G.; Hadley, M.S.; Hagan, J.J.; Healy, M.A.; Johns, A.J.; King, R.J.; Middlemiss, D.N.; Nash, D.J.; Riley, G.J.; Scott, E.E.; Smith, S.A. and Stemp, G. J. Med. Chem. 1996, 39, 1946-1948.
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11. 1H: δ 0.93 (t, 3H), 1.64 (m, 2H), 1.78 (m, 5H), 2.36 (m, 1H), 2.74 (m, 1H), 2.90-3.40 (m, 9H), 3.67 (m, 1H), 7.13 (d, J = 9 Hz, 1H), 7.19 (t, J = 9 Hz, 1H), 7.29 (d, J = 9 Hz, 1H), 7.41 (m, 1H), 7.50 (t, J =9 Hz, 2H), 7.73 (m, 4H), 7.96 (m, 2H), 8.63 (br m, 1H), 10.11 (br s, 1H). Compound 3j, mpt 101-103 °C; 1H: δ 0.30 (m, 2H), 0.54 (m, 2H), 0.93 (t, 3H), 1.20 (m, 1H), 1.63 (m, 2H), 1.76 (m, 3H), 2.29 (m, 1H), 2.45-2.62 (m, 2H), 2.93-3.45 (m, 10H), 3.63 (m, 1H), 3.81 (d, 2H), 6.70 (d, J = 9 Hz, 1H), 6.75 (d, J = 9 Hz, 1H), 7.09 (t, J = 9 Hz, 1H), 7.41 (m, 1H), 7.50 (t, J = 9 Hz, 2H), 7.74 (m, 4H), 7.94 (d, J = 9 Hz, 2H), 8.59 (m, 1H), 9.48 (br s, 1H).