5-ht3

Anpirtoline hydrochloride (D-16949 hydrochloride) is a novel and potent 5-HT1B receptor agonist and 5-HT3 receptor antagonist with anti-injurious, analgesic, and antidepressant activity, and is used in the study of movement disorders.

ADR-851 free base (ADR 851 free base) is a 5-HT3 receptor antagonist and a novel antiemetic with analgesic activity.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Sevoflurane (Fluoromethyl), a noncompetitive inhibitor of 5-HT3 receptor, acts as a low-soluble inhalation anesthetics.

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent, selective 5-HT3 receptor agonist exhibiting anti-depressive-like effects.

Cyamemazine is an antipsychotic compound with sedative and anxiolytic activity. Cyamemazine is a 5-HT3, 5-HT2A, and 5-HT2C receptor antagonist with Ki values of 12 nM, 1.5 nM, and 75 nM, respectively.

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

1. Scopolamine (Scopine (-)-tropate), a nonselective muscarinic receptor antagonist, induces distinct behaviors of attenuated motility and C-like hyperactivity. 2. Scopolamine can increase acetylcholinesterase activity by was significantly attenuated by RCM treatment. 3. Scopolamine can cause learning and memory impairments and galantamine can reverse the symptom. 4. Scopolamine produces rapid and significant symptom improvement in patients with depression.

Zacopride is a highly potent 5-HT3 receptor antagonist (Kd = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM). It also is a selective IK1 channel agonist.

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist that binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

Norcisapride is a 5-hydroxytryptamine receptor 3 (5-HT3) and (5-hydroxytryptamine receptor 4 (5-HT4) dual agonist used for the treatment of gastrointestinal disorders, orofacial disorders, and otorhinolaryngologic disorders.

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

Ticalopride is a 5-HT3 receptor agonist used in the treatment of digestive disorders, orofacial disorders, otorhinolaryngologic disorders, and may be used in the study of bulimia nervosa, gastroesophageal reflux, and irritable bowel syndrome.

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound that acts as a 5-HT3 receptor antagonist, counteracting 5-HT3 agonist and 2-methyl-5-HT, and demonstrating an anti-depressant effect in mice [1].

5-HT3-In-1 (compound example 8) exhabits with 5-HT3 inhibition activity.

5-HT3 antagonist 2 is an antagonist of 5-HT3 receptor.

5-HT3 antagonist 1 is a potent and selective inhibitor of the 5-HT3 receptor.

Erastin is an iron death activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5 0.57 0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.