Synthesis, radiolabeling, and preliminary biological evaluation of [ 3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl] -4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X 7 receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 22, 2004, Pages 5709-5712

  Romagnoli, Romeo ^a   Baraldi, Pier Giovanni ^a   Pavani, Maria Giovanna ^a   Tabrizi, Mojgan Aghazadeh ^a   Moorman, Allan R ^b   Di Virgilio, Francesco ^a   Cattabriga, Elena ^a   Pancaldi, Cecilia ^a   Gessi, Stefania ^a   Borea, Pier Andrea ^a  

^a UNIVERSITY OF FERRARA   (Italy)

^b King Pharmaceuticals   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [N,O BIS(ISOQUINOLINESULFONYL) N METHYLTYROSYL] 4 (2 TOLYL)PIPERAZINE H 3; PIPERAZINE DERIVATIVE; PURINE P2X7 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; RADIOLIGAND; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG SYNTHESIS; EMBRYO; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IC 50; ISOTOPE LABELING; LIGAND BINDING;

ARYLSULFONATES; BINDING SITES; DRUG DESIGN; EVALUATION STUDIES; HUMANS; ISOTOPE LABELING; LIGANDS; MOLECULAR STRUCTURE; RECEPTORS, PURINERGIC P2; STRUCTURE-ACTIVITY RELATIONSHIP; TRITIUM; TYROSINE;

EID: 5144224076     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.07.095     Document Type: Article

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18. 3) δ: 2.21 (s, 3H), 2.33 (m, 1H), 2.52 (dd, J = 12 and 4.2 Hz, 1H), 2.65 (m, 2H), 3.04 (s, 3H), 3.28 (m, 2H), 3.56 (m, 4H), 5.14 (dd, J = 10.2 and 4.4 Hz, 1H), 6.58 (d, J = 8.4 Hz, 1H), 6.82 (d, J = 8.6 Hz, 2H), 7.00 (d, J = 8.6 Hz, 2H), 7.48 (t, J = 7.8 Hz, 1H), 7.51 (s, 1H), 7.59 (t, J = 7.8 Hz, 1H), 7.71 (t, J = 7.8 Hz, 1H), 8.33 (dt, J = 8.4 and 6.0 Hz, 4H), 8.43 (d, J = 6.0 Hz, 1H), 8.52 (d, J = 6.0 Hz, 1H), 8.69 (d, J = 6.0 Hz, 1H), 8.84 (d, J = 6.0 Hz, 1H), 9.36 (s, 1H), 9.43 (s, 1H)