Drug or Compound | Species | Receptor Subtype | Ki, IC50, or EC50 | Main Effect, Application, or Therapeutic Use | Reference |
---|---|---|---|---|---|
Agonist | |||||
5-HT | — | 5-HT3A | 1.56–3.4 µM | Neurotransmitter | Thompson and Lummis, 2003 |
N1E-115a | — | 1.8 µM | Hussy et al., 1994 | ||
SCG (mouse) | — | 2.6 µM | Hussy et al., 1994 | ||
NG108-15b | 5-HT3A | 3.5 µM | Hussy et al., 1994 | ||
Humanc | 5-HT3A | 123 nM | Hope et al., 1996 | ||
Rat | — | 219 nM | Steward et al., 1995 | ||
2-Methyl-5-HT | N1E-115a | — | 11 µM | Derivative of serotonin | Hussy et al., 1994 |
SCG (mouse) | — | 11.8 µM | Hussy et al., 1994 | ||
NG108-15b | 5-HT3A | 13 µM | Hussy et al., 1994 | ||
Humanc | 5-HT3A | 224 nM | Hope et al., 1996 | ||
Humanc | 5-HT3A | 4.1 µM | Davies et al., 1999 | ||
Rat | — | 562 nM | Steward et al., 1995 | ||
m-CPBG | Moused | 5-HT3A | 400 nM | Pharmacological tool | Downie et al., 1994 |
Humanc | 5-HT3A | 19.5 nM | Hope et al., 1996 | ||
Humanc | 5-HT3A | 480 nM | Dubin et al., 1999 | ||
Rat | — | 1.5 nM | Kilpatrick et al., 1990 | ||
Rat | — | 4.77 nM | Steward et al., 1995 | ||
Phenylbiguanide | Moused | 5-HT3A | 18 µM | Pharmacological tool | Downie et al., 1994 |
NG 108-15b | — | 1.2 µM | Dukat et al., 1996 | ||
NG 108-15b | — | 1.8 µM | Downie et al., 1995 | ||
Humanc | 5-HT3A | 2.4 µM | Hope et al., 1996 | ||
Humanc | 5-HT3A | 10.1 µM | Dubin et al., 1999 | ||
Rat | — | 135 nM | Steward et al., 1995 | ||
Varenicline | Humand | 5-HT3A | 5.9 μM | Used for smoking cessation | Lummis et al., 2011 |
Humanc | 5-HT3A | 0.27 μM | |||
Moused | 5-HT3A | 18.3 μM | |||
Humanc | 5-HT3A | 4.9 μM | |||
m-CPP | Mouse | 5-HT3A | 400 nM | Nonselective agonist with psychoactive properties | Downie et al., 1994 |
Humand | 5-HT3A | 480 nM | Dubin et al., 1999 | ||
Humand | 5-HT3A | 19.5 nM | Hope et al., 1996 | ||
Rat | — | 4.77 nM | Steward et al., 1995 | ||
Quipazine | Humand | 5-HT3A | 27 nM | Piperazine analog with antidepressant and oxytocic properties | Dubin et al., 1999 |
Dopamine | Humand | 5-HT3A | 135 μM | Neurotransmitter | Dubin et al., 1999 |
2-Chloro-phenylbiguanide | NG 108-15b | — | 62 nM | — | Dukat et al., 1996 |
3-Chloro-phenylbiguanide | NG 108-15b | — | 17 nM | — | Dukat et al., 1996 |
4-Chloro-phenylbiguanide | NG 108-15b | — | 200 nM | — | Dukat et al., 1996 |
2-Naphthylbiguanide | NG 108-15b | — | 12 nM | — | Dukat et al., 1996 |
2-Methoxy-5-chloro-phenylpiperazine- | NG 108-15b | — | 40 nM | — | Dukat et al., 1996 |
3,4-Dichlorophenylguanidine | NG 108-15b | — | 3.1 nM | — | Glennon et al., 2003 |
3,4,5-Trichlorophenylbiguanide | NG 108-15b | — | 0.7 nM | — | Glennon et al., 2003 |
3,4-Dichlorophenylbiguanide | NG 108-15b | — | 3.1 nM | — | Glennon et al., 2003 |
N-Methylquipazine dimaleate | Rat | — | 4.7 nM | — | Glennon et al., 1989 |
RS 56812 hydrochloride | Rat | — | — | — | Clark et al., 1995 |
SR 57227A | Rat | — | 2.8 nM | Pharmacological tool | Bachy et al., 1993 |
NG 108-15b | — | 250 nM | Bachy et al., 1993 | ||
Competitive antagonists | |||||
Granisetron | Moused | 5-HT3A | 0.14 nM | Antiemetic used for CINV | Downie et al., 1994 |
Humanc | 5-HT3A | 1.44 nM | Hope et al., 1996 | ||
N1E-115a | — | 0.23 nM | Lummis et al., 1993 | ||
Rat | — | 5.13 nM | Steward et al., 1995 | ||
Tropisetron | NG 108-15b | — | 3.85 nM | Antiemetic used for CINV | Downie et al., 1995 |
Rat | — | 4.9 nM | Steward et al., 1995 | ||
Rabbit | — | 0.046 nM | Peters et al., 1993 | ||
Ondansetron | Moused | 5-HT3A | 0.44 nM | Antiemetic used for CINV | Gill et al., 1995 |
Humanc | 5-HT3A | 4.9 nM | Hope et al., 1996 | ||
N1E-115a | — | 7.4 nM | Lummis et al., 1990 | ||
Mouse (NCB-20 cells) | — | 0.25 nM | Lambert et al., 1989 | ||
Rat | — | 46.8 nM | Steward et al., 1995 | ||
Rabbit | — | 0.057 nM | Peters et al., 1993 | ||
Dolasetron | NG 108-15b | — | 20.03 nM | Antiemetic | Boeijinga et al., 1992 |
Azasetron | Rat | — | 2.9 nM | Antiemetic | Sato et al., 1992 |
Ramosetron | Humanc | — | 0.091 nM | Antiemetic, also used for IBS | Hirata et al., 2007 |
Rat | — | 0.22 nM | Hirata et al., 2007 | ||
Alosetron | Guinea pig | — | 50 nM | Used for IBS-D | Zhai et al., 1999 |
Humanc | — | 0.29 nM | Hirata et al., 2007 | ||
Rat | — | 0.71 nM | Hirata et al., 2007 | ||
Cilansetron | Humanc | — | 0.56 nM | Used for IBS-D | Hirata et al., 2007 |
Rat | — | 0.64 nM | Hirata et al., 2007 | ||
Palonosetron (RS 25259-197) | Guinea pig | — | 5.01 nM | Antiemetic used for delayed CINV | Thompson and Lummis, 2007 |
Indisetron | Rat | — | 1.82 nM | Antiemetic | Taniguchi, 2004 |
Bemesetron (MDL-72222) | N1E-115a | — | 16 nM | Antiemetic | Lummis et al., 1990 |
N1E-115a | — | 3.5 nM | Hussy et al., 1994 | ||
SCG (mouse) | — | 5 nM | Hussy et al., 1994 | ||
NG108-15b | 5-HT3A | 3.5 nM | Hussy et al., 1994 | ||
Rat | — | 30.2 nM | Steward et al., 1995 | ||
Rabbit | — | 0.33 nM | Peters et al., 1993 | ||
Mirtazapine | Humanc | 5-HT3A | 2.9 nM | Atypical antidepressant | Eisensamer et al., 2003 |
Zacopride | Human | — | 0.38 nM | Antiemetic, gastroprokinetic, and anxiolytic | Nagakura et al., 1999 |
(S)-Zacopride | Rat | — | 0.95 nM | Steward et al., 1995 | |
(R)-Zacopride | Rat | — | 10.9 nM | Steward et al., 1995 | |
Renzapride | Rat | — | 67.6 nM | Antiemetic | Steward et al., 1995 |
Clozapine | Rat | — | 269 nM | Atypical antipsychotic | Steward et al., 1995 |
Chloroquine | Humand | 5-HT3A | 24.3 μM | Antimalarial agent | Thompson and Lummis, 2008 |
Mefloquine | Humand | 5-HT3A | 0.66 μM | Thompson and Lummis, 2008 | |
Quinine | Humand | 5-HT3A | 1.06 μM | Thompson and Lummis, 2008 | |
Diltiazem | N1E-115a | 5-HT3A | 5.5 nM | L-type calcium channel blocker, used for hypertension, angina, and some heart arrhythmias | Gunthorpe and Lummis, 1999 |
Humand | 5-HT3A | 21 µM | Thompson et al., 2011a | ||
(+)-Verapamil | N1E-115a | 5-HT3A | 2.6 nM | Hargreaves et al., 1996 | |
(−)-Verapamil | N1E-115a | 5-HT3A | 13.1 nM | Hargreaves et al., 1996 | |
Cannabidiol | Humand | 5-HT3A | 0.6 nM | Nonpsychotropic cannabinoid | Yang et al., 2010 |
Poria cocos triterpenoids | Humand | 5-HT3A | 3 nM | Medicinal plant used for chronic gastritis, edema, nephritis, nausea, and emesis | Lee et al., 2009 |
Boldine | Humanc | 5-HT3A | 5.5 µM | Aporphine alkaloid from Peumus boldus leaves with antioxidant properties | Walstab et al., 2014 |
Humanc | 5-HT3AB | 35.5 µM | Walstab et al., 2014 | ||
Morphine | Humanc | 5-HT3A | 13 µM | Opioid analgesic | Baptista-Hon et al., 2012 |
Humanc | 5-HT3AB | 8 µM | Baptista-Hon et al., 2012 | ||
Scopolamine | Humanc | 5-HT3A | 2.09 μM | Muscarinic antagonist used for postoperative nausea and vomiting and motion sickness | Lochner and Thompson, 2016 |
Atropine | Humanc | 5-HT3A | 1.74 μM | Muscarinic antagonist used as cycloplegic and mydriatic, also for bradycardia | Lochner and Thompson, 2016 |
Quercetin | Humand | 5-HT3A | 64.7 μM | Flavonoid with analgesic, prokinetic, anticonvulsant, sedative, and anxiolytic properties | Lee et al., 2005a |
Noncompetitive antagonists | |||||
Alisol extract | Humand | 5-HT3A | 1.7–35 μM | Traditional medicine with diuretic, hypolipemic, antiatherosclerotic, and antihepatitis B virus properties | Lee et al., 2010 |
Anandamide | Humanc | 5-HT3A | 129.6 nM | Endocannabinoid | Barann et al., 2002 |
Δ9-THC | Humanc | 5-HT3A | 38.4 nM | Main psychoactive component of cannabis | Barann et al., 2002 |
WIN55,212-2 | Humanc | 5-HT3A | 103.5 nM | Synthetic, nonselective cannabinoid | Barann et al., 2002 |
Bilobalide | Humand | 5-HT3A | 468 μM | Noncompetitive antagonist of GABA and glycine receptors | Thompson et al., 2011a |
Humand | 5-HT3AB | 3100 μM | Thompson et al., 2011a | ||
Ginkgolide B | Humand | 5-HT3A | 727 μM | Thompson et al., 2011a | |
Humand | 5-HT3AB | 3900 μM | Thompson et al., 2011a | ||
Picrotoxinin | Humand | 5-HT3A | 11 μM | Thompson et al., 2011a | |
Humand | 5-HT3AB | 62 μM | Thompson et al., 2011a | ||
Picrotoxin | Mousec | 5-HT3A | 41.2 μM | GABAA receptor antagonist | Das and Dillon, 2005 |
Citral | Humand | 5-HT3A | 120 µM | Terpenoid used as flavoring agent | Jarvis et al., 2016 |
Linalool | Humand | 5-HT3A | 141 µM | Jarvis et al., 2016 | |
Eucalyptol | Humand | 5-HT3A | 258 µM | Jarvis et al., 2016 | |
(−)-Menthol | Humanc | 5-HT3A | 179.41 µM | Monoterpene from mentha used as flavoring agent | Walstab et al., 2014 |
Ginger extract | Humanc | 5-HT3A | 74.9 nM | Traditional medicine used for spa | Walstab et al., 2013 |
Humanc | 5-HT3AB | 77.2 nM | Walstab et al., 2013 |
Dashes indicate not identified or not applicable. CINV, chemotherapy-induced nausea and vomiting; IBS-D, diarrhea dominant IBS; m-CPP, meta-chlorophenylpiperazine; SCG, superior cervical ganglion.
↵a Mouse neuroblastoma cells.
↵b Mouse neuroblastoma × rat glioma hybrid cells.
↵c Expressed in human embryonic kidney 293 cells.
↵d Expressed in Xenopus laevis oocytes.