Table 2. K_d, K_i and IC₅₀ Values for 5-HT₃ Receptor Selective Antagonists.

Selective Antagonist	Kd, Ki or IC50	Species	Reference
Tropisetron	11nM ¥	Human*	[2]
LY-278,584	5 nM ¥	Human*	[2]
Y-25130	36 nM ¥	Human*	[2]
Granisetron	230 pM ¥	N1E-115	[136]
Granisetron	140 pM	Mouse§	[135]
Granisetron	1.44 nM	Human*	[137]
Granisetron	5.13 nM	Rat tissue homogenate	[143]
Tropisetron	46 pM ¥	Rabbit nodose ganglion	[138]
Tropisetron	3.85 nM ¥	NG 108-15	[139]
Tropisetron	4.9 nM	Rat tissue homogenate	[143]
Ondansetron	57 pM ¥	Rabbit nodose ganglion	[138]
Ondansetron	440 pM ¥	Mouse*	[140]
Ondansetron	7.4 nM¥	N1E-115	[141]
Ondansetron	0.25 nM ¥	NCB-20	[6]
Ondansetron	4.9 nM	Human*	[137]
Ondansetron	46.8 nM	Rat tissue homogenate	[143]
Bemesetron	330 pM ¥	Rabbit nodose ganglion	[138]
MDL-72222	3.5 nM ¥	N1E-115	[142]
MDL-72222	16 nM ¥	N1E-115	[141]
MDL-72222	30.2 nM	Rat tissue homogenate	[143]
BRL-46470	150 pM ¥	Mouse§	[135]
BRL-46470	1.58 nM	Rat tissue homogenate	[143]
BRL-43694	230 pM ¥	N1E-115	[141]
ICS-205-930	640 pM ¥	N1E-115	[141]
Quipazine	1 nM ¥	N1E-115	[141]
Quipazine	1.1 nM	Rat tissue homogenate	[143]
GR-65630	2.5 nM ¥	N1E-115	[141]
SDZ 206-830	871 pM	Rat tissue homogenate	[143]
(S)-zacopride	955 pM	Rat tissue homogenate	[143]
(R)-zacopride	10.9 nM	Rat tissue homogenate	[143]
Alosetron	3.16 nM	Rat tissue homogenate	[143]
Renzapride	67.6 nM	Rat tissue homogenate	[143]
Clozapine	269 nM	Rat tissue homogenate	[143]
2-(4-methyl-1-piperazine)cyclohexa[c]quinoline	0.23 nM	Rat brain homgenate	[154]
Palonosetron	31.6 nM	Rat cerebral cortex, Rabbit ileal myenteric plexus, Guinea-pig ileal plexus	[152]
Dolasetron	20.03 nM	NG 108-15	[153]

^§Expressed in Xenopus oocytes;

^*Expressed in HEK293 cells;

^aNote that quipazine has been classified as both an agonist and non-selective antagonist;

^¥IC₅₀ values calculated using electrophysiological techniques.