5-ht2b

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Metadoxine (Metadoxil) is a neurotransmitter stimulant.

Cabergoline (FCE-21336) is an ergot derived-dopamine D2-like receptor agonist. It has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).Cabergoline permits rapid and effective hormonal and tumor control by normalizing prolactin-producing pituitary adenomas levels.

CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist with pEC50 values of 9.96 for human 5-HT2C, 7.19 for 5-HT2B, and 6.81 for 5-HT2A receptors.

LY266097 hydrochloride (LY 266097 hydrochloride) is an antagonist of 5-HT2 with pKis of 7.7, 9.8, and 7.6 for human 5-HT2A, 5-HT2B, and 5-HT2C and can be used in studies about depression.

BRL-15572 dihydrochloride (BRL 15573 dihydrochloride) is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors. body to stimulate cAMP, Ca2+, ERK1/2 and Fyn kinase.

MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It effectively crosses the blood-brain barrier (BBB) in mice.

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.

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).

PNU 22394 hydrochloride is a 5-HT2C agonist and partial 5-HT2A/5-HT2B agonist

SB 204741 is a selective 5-HT2B antagonist with high affinity and pKi value of 7.1.

TG6-10-1 is an EP2 antagonist.

Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

Tegaserod is an orally available 5-HT4R agonist and 5-HT2B receptor antagonist with inhibitory effects on various 5-hydroxytryptamine receptors. Tegaserod has antitumor activity and is used in the treatment of irritable bowel syndrome (IBS).

PRX-08066 Maleic acid is the salt form of PRX-08066.PRX-08066 is a 5-HT receptor 2B antagonist with an IC50 of 3.4 nM that induces selective vasodilation of the pulmonary artery.

RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).

Nuciferine ((-)-Nuciferine) is an alkaloid found within the plants Nymphaea caerulea and Nelumbo nucifera. It has a profile of action associated with dopamine receptor blockade.

5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 of 33.4 nM, suitable for studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease, or gastrointestinal disease [1] [2].

5-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. It effectively downregulates the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, significantly reducing cellulose deposition. In a CCl4-induced liver fibrosis mouse model, it decreases the fibrotic area and inhibits the progression of fibrosis. This compound is useful for research into immune-inflammatory related diseases, particularly pulmonary fibrosis.

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.