==Effects==When the receptor is activated to open the ion channel by agonists, the following effects are observed:* CNS: nausea and vomiting center in brain stem, anxiety, seizure propensity* PNS: neuronal excitation (in autonomic, nociceptive neurons), emesis==Agonists==Agonists for the receptor include:* 2-methyl-5-HT* Ethanol* Alpha-Methyltryptamine* Ibogaine* Bufotenin* Varenicline* Chlorophenylbiguanide* Quipazine* RS-56812: Potent and selective 5-HT3 partial agonist, 1000x selectivity over other serotonin receptors* SR-57227* YM-31636==Antagonists==Antagonists for the receptor (sorted by their respective therapeutic application) include:* Antiemetics** AS-8112** Granisetron** Ondansetron** Tropisetron* Gastroprokinetics** Alosetron** Batanopride** Metoclopramide (high doses)** Renzapride** Zacopride** M1, the major active metabolite of mosapride* Antidepressants** Mianserin** Mirtazapine** Vortioxetine* Antipsychotics** Clozapine** Olanzapine** Quetiapine* Others** Lamotrigine (Epilepsy and Bipolar Disorder)** Memantine (Alzheimer's disease medication)** Menthol** 3-Tropanyl indole-3-carboxylate==Positive Allosteric Modulators==These agents are not agonists at the receptor, but increase the affinity or efficacy of the receptors for an agonist:* 5-chloroindole==Discovery==Identification of the 5-HT3 receptor did not take place until 1986 because of a lack of selective pharmacological tool.
== Effects ==When the receptor is activated to open the ion channel by agonists, the following effects are observed:* CNS: nausea and vomiting center in brain stem, anxiety, seizure propensity* PNS: neuronal excitation (in autonomic, nociceptive neurons), emesis== Agonists ==Agonists for the receptor include:* 2-methyl-5-HT* Ethanol* Alpha-Methyltryptamine* Ibogaine* Bufotenin* Varenicline* Chlorophenylbiguanide* Quipazine* RS-56812: Potent and selective 5-HT3 partial agonist, 1000x selectivity over other serotonin receptors* SR-57227* YM-31636== Antagonists ==Antagonists for the receptor (sorted by their respective therapeutic application) include:* Antiemetics** AS-8112** Granisetron** Ondansetron** Tropisetron* Gastroprokinetics** Alosetron** Batanopride** Metoclopramide (high doses)** Renzapride** Zacopride** M1, the major active metabolite of mosapride* Antidepressants** Mianserin** Mirtazapine** Vortioxetine* Antipsychotics** Clozapine** Olanzapine** Quetiapine* Others** Lamotrigine (Epilepsy and Bipolar Disorder)** Memantine (Alzheimer's disease medication)** Menthol** 3-Tropanyl indole-3-carboxylate== Positive Allosteric Modulators ==These agents are not agonists at the receptor, but increase the affinity or efficacy of the receptors for an agonist:* 5-chloroindole== Discovery ==Identification of the 5-HT3 receptor did not take place until 1986 because of a lack of selective pharmacological tool.