Novel arylpiperazines as selective α1-adrenergic receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 10, Issue 10, 2000, Pages 1093-1096

  Li, Xiaobing ^a   Murray, William V ^b   Jolliffe, Linda ^b   Pulito, Virginia ^b  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

^b R W JOHNSON PHARMACEUTICAL RES I   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADRENERGIC RECEPTOR BLOCKING AGENT; ALPHA 1A ADRENERGIC RECEPTOR;

ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; NONHUMAN; PROSTATE; RAT;

ADRENERGIC ANTAGONISTS; ANIMALS; BIOCHEMISTRY; CELL MEMBRANE; COS CELLS; DRUG EVALUATION, PRECLINICAL; HUMANS; MALE; MUSCLE CONTRACTION; MUSCLE, SMOOTH; PIPERAZINES; PIPERIDINES; PROSTATE; RATS; RECEPTORS, ADRENERGIC, ALPHA-1; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 0034658091     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(00)00169-4     Document Type: Article

References (5)

1. Harrison J.K., Pearson W.R., Lynch K.R. Trends Pharmacol. Sci. 12:1991;62.
2. Goetz A.S., King H.K., Ward S.D., True T.A., Rimele T.J., Saussy D.L. Jr. Eur. J. Pharmacol. 272:1995;R5.
3. 3): δ 6.89 (m, 4H), 6.68 (bs, 1H), 4.58 (m, 1H), 4.01 (s, 2H), 3.38 (m, 4H), 3.10 (bs, 4H), 2.63 (bs, 4H), 2.54 (t, J=6.1 Hz, 2H), 2.43 (m, 2H), 1.82 (m, 4H), 1.33 (d, J=6.1 Hz, 6H). MS m/z (MH+) 403.
4. Swern D., Mancuso A.J., Huang S.-L. J. Org. Chem. 43:1978;2480.
5. Pulito,V. L.; Li, X.; Varga, S. S.; Mulcahy, L. S.; Clark, K. S.; Pekow, C. A.; Halbert, S. A.; Reitz, A. B.; Murray, W. V.; Jolliffe, L. K. An investigation of the uroselective properties of four novel Alpha-1a adrenoceptor subtype-selective antagonists. J. Pharmacol. Exp. Ther., in press.