Conversion of acyclic nonpeptide CCK antagonists into CCK agonists

被引:4
|
作者
Hirst, GC
Queen, KL
Sugg, EE
Willson, TM
机构
[1] GLAXO WELLCOME INC,RES & DEV,DEPT MED CHEM,RES TRIANGLE PK,NC 27709
[2] GLAXO WELLCOME INC,RES & DEV,DEPT RECEPTOR BIOCHEM,RES TRIANGLE PK,NC 27709
关键词
D O I
10.1016/S0960-894X(97)00062-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The CCK antagonists RP 69758 and (R)-lorglumide were converted into CCK agonists by the introduction of an N-isopropylanilide agonist ''trigger.'' The common structural features of these ligands suggest that nonpeptide agonists and antagonists bind to a common site in the CCK receptor. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:511 / 514
页数:4
相关论文
共 50 条
  • [21] The inability of CCK to block (or CCK antagonists to substitute for) the stimulus effects of chlordiazepoxide
    Fox, MA
    Levine, ES
    Riley, AL
    PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 2001, 69 (1-2) : 77 - 84
  • [22] CHOLECYSTOKININ DIPEPTOID ANTAGONISTS - DESIGN, SYNTHESIS, AND ANXIOLYTIC PROFILE OF SOME NOVEL CCK-A AND CCK-B SELECTIVE AND MIXED CCK-A CCK-B ANTAGONISTS
    BODEN, PR
    HIGGINBOTTOM, M
    HILL, DR
    HORWELL, DC
    HUGHES, J
    REES, DC
    ROBERTS, E
    SINGH, L
    SUMANCHAUHAN, N
    WOODRUFF, GN
    JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (05) : 552 - 565
  • [23] Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases
    Berna, Marc J.
    Jensen, Robert T.
    CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2007, 7 (12) : 1211 - 1231
  • [24] A NEW SIMPLE MOUSE MODEL FOR THE INVIVO EVALUATION OF CHOLECYSTOKININ (CCK) ANTAGONISTS - COMPARATIVE POTENCIES AND DURATIONS OF ACTION OF NONPEPTIDE ANTAGONISTS
    LOTTI, VJ
    CERINO, DJ
    KLING, PJ
    CHANG, RSL
    LIFE SCIENCES, 1986, 39 (18) : 1631 - 1638
  • [25] HIGH-AFFINITY CCK-A AGONISTS BASED ON CCK-4
    LIN, CW
    SHIOSAKI, K
    BIANCHI, BR
    MILLER, TR
    WITTE, DG
    WOLFRAM, CAW
    CRAIG, R
    KOPECKA, H
    WAGENAAR, F
    NADZAN, AM
    FASEB JOURNAL, 1991, 5 (05): : A1227 - A1227
  • [26] CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists
    Pierson, ME
    Comstock, JM
    Simmons, PD
    Julien, R
    Kaiser, F
    Rosamond, JD
    JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (12) : 2350 - 2355
  • [27] Identification of a series of CCK-2 receptor nonpeptide agonists: Sensitivity to stereochemistry and a receptor point mutation
    Kopin, AS
    McBride, EW
    Chen, C
    Freidinger, RM
    Chen, D
    Zhao, CM
    Beinborn, M
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2003, 100 (09) : 5525 - 5530
  • [28] CYCLIC-NUCLEOTIDE ANTAGONISTS OF CCK - STRUCTURAL REQUIREMENTS FOR INTERACTION WITH THE CCK RECEPTOR
    BARLAS, N
    JENSEN, RT
    GARDNER, JD
    GASTROENTEROLOGY, 1980, 78 (05) : 1136 - 1136
  • [29] COMPARISON OF THE INTERACTION OF CCK RECEPTOR ANTAGONISTS WITH CCK RECEPTORS ON GALLBLADDER MUSCLE AND PANCREAS
    VONSCHRENCK, T
    MORAN, TH
    HEINZERIAN, P
    GARDNER, JD
    JENSEN, RT
    GASTROENTEROLOGY, 1987, 92 (05) : 1684 - 1684
  • [30] NEUROCHEMICAL ACTIONS OF CCK UNDERLYING THE THERAPEUTIC POTENTIAL OF CCK-B ANTAGONISTS
    HUGHES, J
    HUNTER, JC
    WOODRUFF, GN
    NEUROPEPTIDES, 1991, 19 : 85 - 89