5-HT Receptor Inhibitor

EMD 86006 is a candidate for selective serotonin inhibitors. EMD 86006 has the potential for research on depressive disorders.

(R)-Citalopram-d₄ (oxalate) is deuterium labeled (R)-Citalopram Oxalate. (R)-Citalopram oxalate, a R-(-) enantiomers of Citalopram (HY-121203), is a serotonin reuptake inhibitor. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate can be used for research of depression.

A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC₅₀ = 13 nM; K_i = 3.8 nM) and α₂-Adrenoceptor receptor antagonist (K_i = 2 nM). A 80426 shows weak antagonistic effect to dopamine D₁ receptor (K_i = 744 nM) and D₂ receptor (K_i = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression.

Benzoctamine hydrochloride (Ba-30803) is a psychoactive agent with anti-anxiety effect. Benzoctamine hydrochloride blocks the central postsynaptic serotonin receptors and decreases 5-HT turnover in the brain.

Bicifadine is an orally active serotonin/norepinephrine/dopamine triple reuptake inhibitor. Bicifadine is an effective antinociceptive in several models of acute, persistent, and chronic pain.

LR1143 is a dopamine transporter (DAT) and 5-HT uptake inhibitor, with IC₅₀ values of 3.4 nM and 112 nM in rats, respectively. LR1143 binds to DAT labeled with the dopamine reuptake inhibitor GBR 12935 (HY-12242A), with an IC₅₀ of 4.4 nM. LR1143 shows lower selectivity for DAT than for serotonin reuptake sites. LR1143 can be used in studies related to cocaine abuse.

Escholtzine perchlorate is an Alkaloid. Escholtzine perchlorate can be isolated from Eschscholzia californica. Escholtzine perchlorate is a CYP3A4 inhibitor, 5-HT_1A receptor inhibitor with a CYP3A4 IC₅₀ of 13.4 μM, 5-HT_1A EC₅₀ of 11 μM. Escholtzine perchlorate can be used for the research of anxiety, depression.

Paroxetine-d6-1 (BRL29060-d6-1) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC₅₀ of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models.

Perphenazine-d₈ (dihydrochloride) is the deuterium labeled Perphenazine, which is a typical antipsychotic agent(5-HT, Dopamine receptor ligand).

Gentisein (Standard) is the analytical standard of Gentisein. This product is intended for research and analytical applications. Gentisein (NSC 329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM.

WAY-100635 (maleate) (Standard) is the analytical standard of WAY-100635 (maleate). This product is intended for research and analytical applications. WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.

Arbortristoside A is an orally active inhibitor of prostaglandin (prostaglandin), histamine (histamine) and serotonin (serotonin). Arbortristoside A mediates anti-inflammatory, analgesic, anti-allergic, immunomodulatory, antiviral and anti-ulcerogenic effects, and also exhibits in vitro anticancer activity. Arbortristoside A can be used in research related to human hepatocellular carcinoma, breast cancer, fibrosarcoma, leishmaniasis, allergic diseases, viral infections and gastric ulcers.

4-CAB hydrochloride is an analog of p-chloroamphetamine, a psychoactive compound which inhibits the reuptake of serotonin (IC₅₀ = 330 nM) and dopamine (IC₅₀ = 2.3 μM).

(R)-Indeloxazine benzenesulfonate (AS1069562) is an orally active 5-HT and NE reuptake inhibitor, with IC₅₀ values of 0.35 μM and 3.3 μM, respectively. (R)-Indeloxazine benzenesulfonate (AS1069562) possesses curative-like analgesic effect. (R)-Indeloxazine benzenesulfonate (AS1069562) might improve nerve function impairment via the amelioration of neurotrophic support.

Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

Femoxetine is a serotonin (5-HT) inhibitor with antidepressant properties. Femoxetine 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 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.

Jatrorrhizine chloride (Standard) is the analytical standard of Jatrorrhizine chloride. This product is intended for research and analytical applications. Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.

5-IAI hydrochloride is a psychoactive analog of p-iodoamphetamine and is indistinguishable, in its physiological effects. 5-IAI hydrochloride significantly reduces both serotonin uptake sites and hippocampal serotonin levels in rats.

Paroxetine (BRL29060) acetate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine acetate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine acetate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine acetate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.