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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1622
    Cyproheptadine
    		Antagonist 99.86%
    Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders.
    Cyproheptadine
  • HY-109157
    Ralmitaront
    		Agonist 99.92%
    Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.
    Ralmitaront
  • HY-101365A
    RS-102221 hydrochloride
    		Antagonist 99.33%
    RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats.
    RS-102221 hydrochloride
  • HY-16978
    TG6-10-1
    		Antagonist 99.92%
    TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.
    TG6-10-1
  • HY-A0008
    Talipexole dihydrochloride
    		Antagonist 99.80%
    Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
    Talipexole dihydrochloride
  • HY-B0002A
    Ondansetron hydrochloride dihydrate
    		Antagonist 99.94%
    Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery.
    Ondansetron hydrochloride dihydrate
  • HY-90003A
    Tianeptine sodium salt
    		Agonist 99.90%
    Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt suppresses MMP-9 via suppression of the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities.
    Tianeptine sodium salt
  • HY-B0032
    Lurasidone Hydrochloride
    		Modulator 99.96%
    Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
    Lurasidone Hydrochloride
  • HY-112390A
    Syk Inhibitor II
    		Inhibitor 98.15%
    Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
    Syk Inhibitor II
  • HY-13788
    LY 344864
    		Agonist 98.93%
    LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.
    LY 344864
  • HY-102064
    SR 57227A
    		Agonist 99.86%
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
    SR 57227A
  • HY-17407
    Ziprasidone hydrochloride monohydrate
    		Antagonist 98.11%
    Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
    Ziprasidone hydrochloride monohydrate
  • HY-W131725
    (+)-Norfenfluramine
    		Agonist 98.79%
    (+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease.
    (+)-Norfenfluramine
  • HY-156601
    Bexicaserin
    		Agonist 99.96%
    Bexicaserin (LP352) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related disorders (such as epilepsy).
    Bexicaserin
  • HY-19733
    Lumateperone tosylate
    		Antagonist 99.53%
    Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
    Lumateperone tosylate
  • HY-U00096
    Ansofaxine hydrochloride
    		Inhibitor 99.72%
    Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
    Ansofaxine hydrochloride
  • HY-16688
    RU 24969
    		Agonist 99.77%
    RU 24969 is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.
    RU 24969
  • HY-B1154
    Penbutolol sulfate
    		Antagonist 98.72%
    Penbutolol sulfate ((-)-Terbuclomine) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3.
    Penbutolol sulfate
  • HY-123205
    Oxatomide
    		Inhibitor 99.56%
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
    Oxatomide
  • HY-B0072
    Tropisetron
    		Antagonist 98.72%
    Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.
    Tropisetron
Cat. No. Product Name / Synonyms Application Reactivity