Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D3 receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 11, 1996, Pages 1233-1236

  Bolton, David ^a   Boyfield, Izzy ^a   Coldwell, Martyn C ^a   Hadley, Michael S ^a   Healy, Maureen A M ^a   Johnson, Christopher N ^a   Markwell, Roger E ^a   Nash, David J ^a   Riley, Graham J ^a   Stemp, Geoffrey ^a   Wadsworth, Harry J ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

DOPAMINE 3 RECEPTOR; DOPAMINE 3 RECEPTOR BLOCKING AGENT; PYRROLE DERIVATIVE;

ARTICLE; BINDING AFFINITY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; RECEPTOR AFFINITY; SCHIZOPHRENIA;

EID: 0029953237     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00202-8     Document Type: Article

References (7)

1. Seernan, P. Synapse. 1987, 1, 133-152.
2. Grandy, D. K.; Marchionni, M. A.; Makam, H.; Stofko, R. E.; Alfano, M.; Frothingham, L.; Fischer, J. B.; Burke-Howie, K. J.; Bunzow, J. R.; Server, A. C.; Civelli, O. Proc. Nat. Acad. Sci. 1989, 86, 9762-9766.
3. Sokoloff, P.; Giros, B.; Martres, M-P.; Bouthenet, M-L.; Schwarte, J-C. Nature. 1990, 347, 146-151.
4. Van Tol, H. H. M.; Bunzow, J. R.; Guan, H-C.; Sunahara, R. K.; Seeman, P.; Niznik, H. B.; Civelli, O. Nature. 1991, 350, 610-614.
5. van Wijngaarden, I.; Kruse, C. G.; van Hes, R.; van der Heyden, J. A. M.; Tulp, M. T. M. J. Med. Chem. 1987, 30, 2099-2104.
6. 1H (free base): δ 1.19 (t, J=7Hz, 3H), 1.40-1.90 (m, 8H), 2.72 (m, 1H), 2.91 (m, 1H), 3.02 (q, J=7Hz, 2H), 3.43 (d, J=14Hz, 1H), 3.53 (d, J=14Hz, 1H), 3.66 (m, 1H), 4.00 (s, 3H), 5.93 (t, J=3Hz, 1H), 6.52 (m, 1H), 7.01 (d, J=9Hz, 1H), 7.24 (m, 1H), 7.26 (m, 2H), 7.38 (m, 2H), 7.55 (m, 1H), 7.99 (d, J=2Hz, 1H), 9.6 (br s, 1H).
7. 3 receptor of 7.7 and 9.7, respectively.