THE SYNTHESIS AND CCK RECEPTOR AFFINITIES OF SELECTED CARBOXYLIC-ACID MIMICS OF CL-988 - A POTENT AND SELECTIVE CCK-B ANTAGONIST

被引:5
作者
DRYSDALE, MJ
PRITCHARD, MC
HORWELL, DC
机构
[1] Parke Davis Neuroscience Research Centre, Addenbrookes Hospital Site, Cambridge, CB22 2QB, Hills Rd
关键词
D O I
10.1016/S0960-894X(00)80652-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Syntheses of selected acid mimics of the CCK-B selective receptor antagonist CI-988 (1) are described. The relationship between pK(a) and CCK-B binding affinities of these compounds are discussed.
引用
收藏
页码:45 / 48
页数:4
相关论文
共 16 条
[1]   BEHAVIORAL AND NEUROPHYSIOLOGICAL EVIDENCE FOR A FACILATORY INTERACTION BETWEEN CO-EXISTING TRANSMITTERS - CHOLECYSTOKININ AND DOPAMINE [J].
CRAWLEY, JN ;
HOMMER, DW ;
SKIRBOLL, LR .
NEUROCHEMISTRY INTERNATIONAL, 1984, 6 (06) :755-760
[2]   PSYCHOPHARMACOLOGICAL PROFILE OF CHOLECYSTOKININ USING THE SELF-STIMULATION AND THE DRUG DISCRIMINATION PARADIGMS [J].
DEWITTE, P ;
SWANET, E ;
GEWISS, M ;
GOLDMAN, S ;
ROQUES, B ;
VANDERHAEGHEN, JJ .
ANNALS OF THE NEW YORK ACADEMY OF SCIENCES, 1985, 448 (JUL) :470-487
[3]   THE DISCOVERY OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - A NEW CLASS OF POTENT ANTIHYPERTENSIVES [J].
DUNCIA, JV ;
CHIU, AT ;
CARINI, DJ ;
GREGORY, GB ;
JOHNSON, AL ;
PRICE, WA ;
WELLS, GJ ;
WONG, PC ;
CALABRESE, JC ;
TIMMERMANS, PBMWM .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (05) :1312-1329
[4]  
EDEN JM, 1991, UNPUB J MED CHEM
[5]   STRUCTURAL, CONFORMATIONAL, AND STEREOCHEMICAL REQUIREMENTS OF CENTRAL EXCITATORY AMINO-ACID RECEPTORS [J].
HANSEN, JJ ;
KROGSGAARDLARSEN, P .
MEDICINAL RESEARCH REVIEWS, 1990, 10 (01) :55-94
[6]  
HAYWARD NJ, 1991, IN PRESS BR J PHARM
[7]   RATIONALLY DESIGNED DIPEPTOID ANALOGS OF CCK - ALPHA-METHYLTRYPTOPHAN DERIVATIVES AS HIGHLY SELECTIVE AND ORALLY ACTIVE GASTRIN AND CCK-B ANTAGONISTS WITH POTENT ANXIOLYTIC PROPERTIES [J].
HORWELL, DC ;
HUGHES, J ;
HUNTER, JC ;
PRITCHARD, MC ;
RICHARDSON, RS ;
ROBERTS, E ;
WOODRUFF, GN .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (01) :404-414
[8]  
JENSEN RT, 1982, J BIOL CHEM, V257, P5554
[9]  
JORPES JE, 1973, SECRETIN CHOLECYSTOK, P1
[10]  
Lipinski C. A., 1986, ANNU REP MED CHEM, V21, P283