Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron).
Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron).
复制标题
BRL 43694（格拉司琼）具有选择性和功能性 5-羟色胺 3 受体拮抗作用。
DOI：
10.1016/0014-2999(89)90695-x
复制
发表时间：
1989
影响因子：
5
通讯作者：
D. Nelson
中科院分区：
文献类型：
--
作者：
G. Sanger;D. Nelson
The activity of BRL 43694 (granisetron) was investigated using established models of 5-HT3receptor activity. In guinea-pig isolated ileum. BRL 43694 antagonised the contractions evoked by relatively high concentrations of 5-HT (pA2= 8.1 ± 0.2). However, except in high concentrations, BRL 43694 did not affect the contractions of similar preparations of ileum, evoked by electrical field stimulation (cholinergically mediated), the nicotinic agonist dimethylphenyl piperazinium (DMPP) or by cholecystokinin octapeptide. Similarly, BRL 43694 did not affect electrically evoked, cholinergically mediated contractions of rat or human isolated stomach. In other models of 5-HT3receptor activity (rabbit isolated heart, Bezold-Jarisch reflex in anaesthetised rats), potent antagonism by BRL 43694 was demonstrated. In radioligand binding studies on rat brain membranes, BRL 43694 had little or no affinity for 5-HT1A, 5-HT1B, 5-HT2or for many other binding sites. BRL 43694 may therefore be a potent and selective 5-HT3receptor antagonist.
[3H]quipazine 标记大鼠皮质膜中的 5-HT3 识别位点。
影响因子：
5
作者：
Peroutka,SJ;Hamik,A
通讯作者：
Hamik,A