5-ht2a receptor

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

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.

Org-12962 is an effective and selective 5-HT2C receptor agonist pEC50: 7.01). Org-12962 shows antiaversive effects in a rat model of panic-like anxiety. Org-12962 also shows high effacy for the 5-HT2A and 5-HT2B receptors (pEC50s: 6.38 and 6.28, respectively).

5-HT6 5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

Compound 42, a 5-HT6 5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor, specifically stimulating the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors with EC50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].

5-HT2A receptor agonist-6 (compound 47) is a selective agonist of the 5-HT2A receptor with a pEC50 value of 6.58.

5-HT2A receptor agonist-5 (compound I-3) is a potent 5-HT2A agonist with a Ki value of 0.017 µM and exhibits antidepressant activity.

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

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.

(-)-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.

Acetylcysteine (NAC) is an N-acetyl derivative of cysteine, a ROS inhibitor and mucolytic agent. Acetylcysteine induces apoptosis, can be used to reduce mucus thickness, and has anti-influenza viral activity.

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.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1 4 5 6. Empagliflozin is used for the treatment of type 2 diabetes.

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.