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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

Related Products

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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-14763S
    Cariprazine-d6
    		Modulator 98.00%
    Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM).
    Cariprazine-d<sub>6</sub>
  • HY-151596
    MAO-A/5-HT2AR-IN-1
    		Inhibitor 99.71%
    MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent.
    MAO-A/5-HT2AR-IN-1
  • HY-B1517AR
    Alprenolol hydrochloride (Standard)
    		Antagonist
    Alprenolol (hydrochloride) (Standard) is the analytical standard of Alprenolol (hydrochloride). This product is intended for research and analytical applications. Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
    Alprenolol hydrochloride (Standard)
  • HY-103135
    SB 206553 hydrochloride
    		Antagonist 99.36%
    SB 206553 hydrochloride is a high affinity, selective and orally active 5-HT2B / 5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92). SB 206553 possesses anxiolytic-like properties.
    SB 206553 hydrochloride
  • HY-12537
    Peptide 401
    		Antagonist 98.26%
    Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
    Peptide 401
  • HY-110094
    BIMU 8
    		Agonist 99.60%
    BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors.
    BIMU 8
  • HY-103430
    SKF-83566 hydrobromide
    		Antagonist
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.
    SKF-83566 hydrobromide
  • HY-101343
    RS 39604
    		Antagonist ≥98.0%
    RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites.
    RS 39604
  • HY-100970
    4F 4PP oxalate
    		Antagonist 98.86%
    4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM).
    4F 4PP oxalate
  • HY-W100249
    MMAI
    		Activator 99.08%
    MMAI is a selective serotonin releaser that can be used in the research of mental illnesses.
    MMAI
  • HY-N0749
    Jatrorrhizine
    		Inhibitor
    Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
    Jatrorrhizine
  • HY-103112A
    SB 243213 dihydrochloride
    		Antagonist ≥99.0%
    SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
    SB 243213 dihydrochloride
  • HY-160921
    Capeserod
    		Agonist 98.66%
    Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models.
    Capeserod
  • HY-10351A
    Robalzotan hydrochloride
    		Inhibitor 99.5%
    Robalzotan hydrochloride (NAD-​299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.
    Robalzotan hydrochloride
  • HY-12714
    TDHL
    		Antagonist
    TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.
    TDHL
  • HY-B0740R
    Cyclobenzaprine hydrochloride (Standard)
    		Antagonist 99.99%
    Cyclobenzaprine (MK130) hydrochloride (Standard) is the analytical standard of Cyclobenzaprine (MK130) hydrochloride. This product is intended for research and analytical applications. Cyclobenzaprine hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases
    Cyclobenzaprine hydrochloride (Standard)
  • HY-103090
    NPS ALX Compound 4a
    		Antagonist ≥99.0%
    NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.
    NPS ALX Compound 4a
  • HY-100243
    (+)-Norcisapride
    		Modulator 99.32%
    (+)-Norcisapride (Ticalopride) is a potent 5-HT4 agonist and a 5-HT3 antagonist. (+)-Norcisapride has activity in animals models of constipation.
    (+)-Norcisapride
  • HY-105201
    Fabesetron
    		Antagonist
    Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
    Fabesetron
  • HY-160887
    FPT
    		Agonist 98.06%
    FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models.
    FPT
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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