DEVELOPMENT OF ANGIOTENSIN-II ANTAGONISTS WITH EQUIPOTENT AFFINITY FOR HUMAN AT(1) AND AT(2) RECEPTOR SUBTYPES

被引:9
作者
GLINKA, TW [1 ]
DELASZLO, SE [1 ]
SIEGL, PKS [1 ]
CHANG, RS [1 ]
KIVLIGHN, SD [1 ]
SCHORN, TS [1 ]
FAUST, KA [1 ]
CHEN, TB [1 ]
ZINGARO, GJ [1 ]
LOTTI, VJ [1 ]
GREENLEE, WJ [1 ]
机构
[1] MERCK SHARP & DOHME LTD,RES LABS,DEPT PHARMACOL,W POINT,PA 19486
关键词
D O I
10.1016/0960-894X(94)85036-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The quinazolinone sulfonylcarbamate L-163,579 (9) is a potent, balanced antagonist of the binding of angiotensin II (Ang II) to human AT(1) and AT(2) receptors. This antagonist produces a long-lasting blockade of Ang II-induced presser response in both rats and dogs after oral administration.
引用
收藏
页码:2337 / 2342
页数:6
相关论文
共 17 条
  • [1] CHANG RSL, 1992, J PHARMACOL EXP THER, V262, P133
  • [2] ORAL-ADMINISTRATION OF DUP-753, A SPECIFIC ANGIOTENSIN-II RECEPTOR ANTAGONIST, TO NORMAL-MALE VOLUNTEERS - INHIBITION OF PRESSOR-RESPONSE TO EXOGENOUS ANGIOTENSIN-I AND ANGIOTENSIN-II
    CHRISTEN, Y
    WAEBER, B
    NUSSBERGER, J
    PORCHET, M
    BORLAND, RM
    LEE, RJ
    MAGGON, K
    SHUM, L
    TIMMERMANS, PBMWM
    BRUNNER, HR
    [J]. CIRCULATION, 1991, 83 (04) : 1333 - 1342
  • [3] QUINAZOLINONES-2 - QSAR AND INVIVO CHARACTERIZATION OF AT1 SELECTIVE AII ANTAGONISTS
    DELASZLO, SE
    ALLEN, EE
    QUAGLIATO, CS
    GREENLEE, WJ
    PATCHETT, AA
    NACHBAR, RB
    SIEGL, PKS
    CHANG, RS
    KIVLIGHN, SD
    SCHORN, TS
    FAUST, KA
    CHEN, TB
    ZINGARO, GJ
    LOTTI, VJ
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (06) : 1299 - 1304
  • [4] A POTENT, ORALLY-ACTIVE, BALANCED AFFINITY ANGIOTENSIN-II AT(1) ANTAGONIST AND AT(2) BINDING INHIBITOR
    DELASZLO, SE
    QUAGLIATO, CS
    GREENLEE, WJ
    PATCHETT, AA
    CHANG, RSL
    LOTTI, VJ
    CHEN, TB
    SCHECK, SA
    FAUST, KA
    KIVLIGHN, SS
    SCHORN, TS
    ZINGARO, GJ
    SIEGL, PKS
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (21) : 3207 - 3210
  • [5] DUNCIA JV, IN PRESS BIORGANIC M
  • [6] A NEW CLASS OF BALANCED AT(1)/AT(2) ANGIOTENSIN-II ANTAGONISTS - QUINAZOLINONE AII ANTAGONISTS WITH ACYLSULFONAMIDE AND SULFONYLCARBAMATE ACIDIC FUNCTIONALITIES
    GLINKA, TW
    DELASZLO, SE
    SIEGL, PKS
    CHANG, RS
    KIVLIGHN, SD
    SCHORN, TS
    FAUST, KA
    CHEN, TB
    ZINGARO, GJ
    LOTTI, VJ
    GREENLEE, WJ
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (01) : 81 - 86
  • [7] GLINKA TW, IN PRESS BIORGANIC M
  • [8] KAMBAYASHI Y, 1993, J BIOL CHEM, V268, P24543
  • [9] MUKOYAMA M, 1993, J BIOL CHEM, V268, P24539
  • [10] POTENT IMIDAZOLE ANGIOTENSIN-II ANTAGONISTS - ACYL SULFONAMIDES AND ACYL SULFAMIDES AS TETRAZOLE REPLACEMENTS
    NAYLOR, EM
    CHAKRAVARTY, PK
    COSTELLO, CA
    CHANG, RS
    CHEN, TB
    FAUST, KA
    LOTTI, VJ
    KIVLIGHN, SD
    ZINGARO, GJ
    SIEGL, PKS
    WONG, PC
    CARINI, DJ
    WEXLER, RR
    PATCHETT, AA
    GREENLEE, WJ
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (01) : 69 - 74