SYNTHESIS AND 5-HT3 RECEPTOR AGONIST ACTIVITY OF ARYLUREAS DERIVED FROM HISTAMINE

被引:5
作者
BERMUDEZ, J [1 ]
BOYLAND, P [1 ]
KING, FD [1 ]
SUMMERSELL, RJ [1 ]
机构
[1] SMITHKLINE BEECHAM PHARMACEUT,COLDHARBOUR RD,HARLOW,ESSEX,ENGLAND
关键词
D O I
10.1016/S0960-894X(01)80877-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of aryl ureas derived from histamine is described. The compounds are shown to be 5-HT3 receptor agonists by their ability to initiate the Bezold-Jarisch reflux and to displace [H-3]-BRL 43694 from central 5-HT3 receptors with a potency equivalent to that of 5-HT.
引用
收藏
页码:205 / 208
页数:4
相关论文
共 10 条
[1]   5-HYDROXYTRYPTAMINE (5-HT3) RECEPTOR ANTAGONISTS .3. ORTHO-SUBSTITUTED PHENYLUREAS [J].
BERMUDEZ, J ;
DABBS, S ;
KING, FD .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (07) :1932-1935
[2]   5-HYDROXYTRYPTAMINE (5-HT3) RECEPTOR ANTAGONISTS .1. INDAZOLE AND INDOLIZINE-3-CARBOXYLIC ACID-DERIVATIVES [J].
BERMUDEZ, J ;
FAKE, CS ;
JOINER, GF ;
JOINER, KA ;
KING, FD ;
MINER, WD ;
SANGER, GJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (07) :1924-1929
[3]   PHARMACOLOGICAL PROPERTIES OF GR38032F, A NOVEL ANTAGONIST AT 5-HT3 RECEPTORS [J].
BUTLER, A ;
HILL, JM ;
IRELAND, SJ ;
JORDAN, CC ;
TYERS, MB .
BRITISH JOURNAL OF PHARMACOLOGY, 1988, 94 (02) :397-412
[4]  
DUNBAR AW, 1986, BRIT J PHARMACOL, V88, pP374
[5]   1-(M-CHLOROPHENYL)-BIGUANIDE, A POTENT HIGH-AFFINITY 5-HT3 RECEPTOR AGONIST [J].
KILPATRICK, GJ ;
BUTLER, A ;
BURRIDGE, J ;
OXFORD, AW .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 182 (01) :193-197
[6]  
KING F D, 1989, Drugs of the Future, V14, P875
[7]   [H-3]-BRL-43694 (GRANISETRON), A SPECIFIC LIGAND FOR 5-HT3 BINDING-SITES IN RAT-BRAIN CORTICAL MEMBRANES [J].
NELSON, DR ;
THOMAS, DR .
BIOCHEMICAL PHARMACOLOGY, 1989, 38 (10) :1693-1695
[8]   IDENTIFICATION OF SEROTONIN M-RECEPTOR SUBTYPES AND THEIR SPECIFIC BLOCKADE BY A NEW CLASS OF DRUGS [J].
RICHARDSON, BP ;
ENGEL, G ;
DONATSCH, P ;
STADLER, PA .
NATURE, 1985, 316 (6024) :126-131
[9]   THE AGONIST PROPERTIES OF META-CHLOROPHENYLBIGUANIDE AND 2-METHYL-5-HYDROXYTRYPTAMINE ON 5-HT3 RECEPTORS IN N1E-115 NEUROBLASTOMA-CELLS [J].
SEPULVEDA, MI ;
LUMMIS, SCR ;
MARTIN, IL .
BRITISH JOURNAL OF PHARMACOLOGY, 1991, 104 (02) :536-540
[10]  
THOMAS D R, 1990, Journal of Psychopharmacology, V4, P289