5-HT Receptor Inhibitor

Adafenoxate is a nootropic agent. Adafenoxate can improve Scopolamine (HY-N0296)-impaired memory, exploratory behavior and physical capabilities. Adafenoxate can be used for the research of neurological disease.

Clovoxamine (DU23811) (Compound 35) has binding affinity for serotonin transporter (SERT) (K_i: 61 nM). Clovoxamine is a 5-HT and norepinephrine reuptake (NE) re-uptake inhibitor. Clovoxamine is an antidepressant.

5-HT2C-agonist-14 is a 5-HT2C receptor agonist with an EC₅₀ of 2.9 μM against human receptors. It also acts as a voltage-gated sodium channel inhibitor with blood-brain barrier permeable. 5-HT2C-agonist-14 elevates seizure threshold, suppresses seizure progression and alleviates pain-related behaviors. It can be used in the research of epilepsy and pain-related diseases.

BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC₅₀ = 101 nM) and serotonin transporter (SERT) (IC₅₀ = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC₅₀ of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC₅₀ = 7.7 μM), L-type calcium channel (IC₅₀ = 3.6 μM), σ receptor (IC₅₀ = 2 μM), and sodium channel (IC₅₀ = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease.

Butriptyline (Butriptylene) hydrochloride is an orally active tricyclic antidepressant that slightly enhances central 5-HT effects. Butriptyline hydrochloride does not inhibit brain norepinephrine uptake. Butriptyline hydrochloride can be used for depression research.

Cianopramine (Cyanimipramine) is a tricyclic antidepressant, and a potent inhibitor of neuronal serotonin (5-HT) uptake. Cianopramine blocks central and peripheral 5-HT receptors.

EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human K_i value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pK_i values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity.

Cyproheptadine hydrochloride-d₃ (Cyproheptadine HCl-d₃) is the d₃-labeled Cyproheptadine (hydrochloride) (HY-B0366A). Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator.

DOV-102,677 is an orally sctive triple monoamine neurotransmitter reuptake inhibitor that simultaneously inhibits the dopamine (DAT) (IC₅₀ = 129 nM; K_i = 222 nM), norepinephrine (NET) (IC₅₀ = 103 nM; K_i = 1030 nM), and serotonin (SERT) (IC₅₀ = 133 nM; K_i = 740 nM) transporters. DOV-102,677 demonstrated significant antidepressant-like activity and sensory-motor gating regulatory effects in mouse experiments. DOV-102,677 can be used for research on depression.

5-Hydroxy-6-methoxy (S)-duloxetine maleate is an orally active and brain-penetrant serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with antidepressant and analgesic activities. 5-Hydroxy-6-methoxy (S)-duloxetine maleate is promising for research of psychiatric and neurological disorders such as depression, diabetic neuropathic pain, generalized anxiety disorder, and fibromyalgia.

Femoxetine hydrochloride is a serotonin (5-HT) inhibitor with antidepressant properties. Femoxetine hydrochloride increases serotonin levels in the brain by preventing serotonin from being reabsorbed by nerve cells, resulting in increased concentrations of the neurotransmitter in the synaptic gap, which enhances serotonin signaling. Femoxetine hydrochloride can be used to study the role of serotonin in depression and other emotional disorders, and how 5-HT reuptake inhibitors affect mood and behavior.

S 15931 is a 5-HT_1A receptor inhibitor. S 15931 inhibits the late-phase hindpaw licking response induced by formalin and the abdominal writhing response induced by acetic acid in Mus musculus. S 15931 abolishes the spontaneous tail-flick response induced by 8-OH-DPAT in Rattus norvegicus and potentiates the analgesic effect of morphine. S 15931 is applicable for pain-related research.

Org 6582 is a competitive, selective, and long-acting 5-HT (K_i = 89 nM) uptake inhibitor. Org 6582’s inhibitory effect on 5-HT uptake can last for more than 48 hours. Org 6582 can be used for research on depressive disorders.

Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect.

MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with K_i of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.

BMS-505130 fumarate is a potent, selective and orally active serotonin transport inhibitor with a K_i for binding to the serotonin transporter of 0.18 nM (K_i for norepinephrine and dopamine transporters of 4.6 and 2.1 μM, respectively). BMS-505130 fumarate can be used for the research of neurological disease, such as depression.

Ifoxetine (CGP 15210G) hemisulfate is an inhibitor of 5-HT reuptake. Ifoxetine hemisulfate specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine hemisulfate inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine hemisulfate has antidepressant properties.

Melitracen (hydrochloride) (Standard) is the analytical standard of Melitracen (hydrochloride). This product is intended for research and analytical applications. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.