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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 02期

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

页码：205 / 208

页数：4

共 50 条

[1] Unbinding pathways of an agonist and an antagonist from the 5-HT3 receptor
Thompson, AJ
Chau, PL
Chan, SL
Lummis, SCR
BIOPHYSICAL JOURNAL, 2006, 90 (06) : 1979 - 1991
[2] TEMPERATURE, FOOD-INTAKE, AND LOCOMOTOR-ACTIVITY EFFECTS OF A 5-HT3 RECEPTOR AGONIST AND 2 5-HT3 RECEPTOR ANTAGONISTS IN RATS
MAZZOLAPOMIETTO, P
AULAKH, CS
MURPHY, DL
PSYCHOPHARMACOLOGY, 1995, 121 (04) : 488 - 493
[3] A new 5-HT3 receptor ligand.: II.: Structure-activity analysis of 5-HT3 receptor agonist action in the gut
Yamada, M
Sato, Y
Kobayashi, K
Konno, F
Soneda, T
Watanabe, T
CHEMICAL & PHARMACEUTICAL BULLETIN, 1998, 46 (03) : 445 - 451
[4] 5-HT3 RECEPTOR AGONIST EFFECTS OF ZACOPRIDE IN THE FERRET
MIDDLEFELL, VC
PRICE, TL
THOMSON, IA
BRITISH JOURNAL OF PHARMACOLOGY, 1990, 101 : P560 - P560
[5] Analgesic activity of 5-HT3 receptor antagonists
Spasov, AA
Chernikov, MV
Kiabiya, ST
BULLETIN OF EXPERIMENTAL BIOLOGY AND MEDICINE, 2005, 139 (04) : 424 - 426
[6] Analgesic Activity of 5-HT3 Receptor Antagonists
A. A. Spasov
M. V. Chernikov
S. T. Kiabiya
Bulletin of Experimental Biology and Medicine, 2005, 139 : 424 - 426
[7] α-thujone reduces 5-HT3 receptor activity by an effect on the agonist-induced desensitization
Deiml, T
Haseneder, R
Zieglgänsberger, W
Baghai, TC
Eser, D
Schüle, C
Ella, R
Eisensamer, B
Rupprecht, R
Hapfelmeier, G
PHARMACOPSYCHIATRY, 2003, 36 (05) : 219 - 219
[8] α-thujone reduces 5-HT3 receptor activity by an effect on the agonist-induced desensitization
Deiml, T
Haseneder, R
Zieglgänsberger, W
Rammes, G
Eisensamer, B
Rupprecht, R
Hapfelmeier, G
NEUROPHARMACOLOGY, 2004, 46 (02) : 192 - 201
[9] Synthesis of the derivatives of tetramethylpyrazine and screening for 5-HT3 receptor antagonistic activity
Jiang, XQ
Huang, CM
Zhu, LP
Ye, DY
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2005, 26 (04): : 683 - 685
[10] Synthesis and pharmacological characterization of a new benzoxazole derivative as a potent 5-HT3 receptor agonist
López-Tudanca, PL
Labeaga, L
Innerárity, A
Alonso-Cires, L
Tapia, I
Mosquera, R
Orjales, A
BIOORGANIC & MEDICINAL CHEMISTRY, 2003, 11 (13) : 2709 - 2714

← 1 2 3 4 5 →