2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

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5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. Type: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics,antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.

5-HT Receptor Isoform Specific Products:

5-HT Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15414R
    Vortioxetine (Standard)
    		Inhibitor
    Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
    Vortioxetine (Standard)
  • HY-14958A
    Pardoprunox hydrochloride
    		Agonist 99.46%
    Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively.
    Pardoprunox hydrochloride
  • HY-15780S1
    Brexpiprazole-d8-1
    Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
    Brexpiprazole-d<sub>8</sub>-1
  • HY-125641
    AL-34662
    		Agonist 99.19%
    AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent.
    AL-34662
  • HY-100649
    Hydroxy ziprasidone
    		Antagonist 99.53%
    Hydroxy ziprasidone is an impurity of Ziprasidone. Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist.
    Hydroxy ziprasidone
  • HY-B0031S
    Quetiapine-d4 fumarate
    		Agonist ≥98.0%
    Quetiapine-d4 (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.
    Quetiapine-d<sub>4</sub> fumarate
  • HY-101924
    AVN-492
    		Antagonist 99.30%
    AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
    AVN-492
  • HY-110033
    Ecopipam hydrobromide
    		Antagonist ≥99.0%
    Ecopipam (SCH 39166) hydrobromide is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrobromide can be used for the research of schizophrenia and obesity.
    Ecopipam hydrobromide
  • HY-19742A
    Lecozotan hydrochloride
    		Antagonist 98.71%
    Lecozotan (SRA-333) hydrochloride is an orally active and selective antagonist of 5-HT1A with a Ki of 4.5 nM for cloned human 5-HT1A receptor. Lecozotan hydrochloride enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. Lecozotan hydrochloride has the potential for mild-to-moderate Alzheimer's disease (AD) research.
    Lecozotan hydrochloride
  • HY-14539S
    Clozapine-d8
    		Modulator 99.68%
    Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.
    Clozapine-d<sub>8</sub>
  • HY-103089
    LY393558
    		Antagonist ≥99.0%
    LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression.
    LY393558
  • HY-14543S
    Sertindole-d4
    		Antagonist 98.64%
    Sertindole-d4 is the deuterium labeled Sertindole. Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.
    Sertindole-d<sub>4</sub>
  • HY-116565
    Usmarapride
    		Modulator ≥98.0%
    Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
    Usmarapride
  • HY-17382B
    Metoclopramide hydrochloride
    		Antagonist 99.96%
    Metoclopramide hydrochloride is a potent and orally active antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
    Metoclopramide hydrochloride
  • HY-B0189B
    Mosapride citrate dihydrate
    		Agonist
    Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.
    Mosapride citrate dihydrate
  • HY-110232
    Risperidone-d4
    		Inhibitor 99.40%
    Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
    Risperidone-d<sub>4</sub>
  • HY-B0965AS
    Thioridazine-d3 hydrochloride
    		Antagonist 99.19%
    Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine-d<sub>3</sub> hydrochloride
  • HY-14848A
    Naluzotan hydrochloride
    		Agonist 99.63%
    Naluzotan hydrochloride is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
    Naluzotan hydrochloride
  • HY-167902
    YM-31636 free base
    		Agonist
    YM-31636 free base is an orally active, potent and selective 5-HT3 receptor agonist with a Ki value of 0.2 nM. YM-31636 free base induces contraction of isolated guinea pig distal colon. YM-31636 free base induces tachycardia with the relative intrinsic activity of approximately 0.23 in isolated guinea pig right atrium. YM-31636 free base is promising for research of constipation.
    YM-31636 free base
  • HY-14547A
    Bifeprunox mesylate
    		Agonist 99.89%
    Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia.
    Bifeprunox mesylate
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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