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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

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-103136
    R-96544
    Antagonist 99.50%
    R-96544 is an orally active 5-HT2A receptor antagonist. R-96544 can inhibit platelet aggregation in vitro.
    R-96544
  • HY-14541S
    Olanzapine-d3
    Antagonist 99.09%
    Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>3</sub>
  • HY-10559
    Nelotanserin
    Antagonist 99.52%
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
    Nelotanserin
  • HY-111419
    DSP-1053
    Agonist 99.75%
    DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity.
    DSP-1053
  • HY-103133
    WAY208466 dihydrochloride
    Agonist 98.43%
    WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex. WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects.
    WAY208466 dihydrochloride
  • HY-110129
    Eplivanserin hemifumarate
    Antagonist 98.07%
    Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
    Eplivanserin hemifumarate
  • HY-14785A
    Befiradol hydrochloride
    Agonist 99.93%
    Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT1A receptor agonist.
    Befiradol hydrochloride
  • HY-117575A
    WAY-100135 dihydrochloride
    Antagonist 98.32%
    WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties.
    WAY-100135 dihydrochloride
  • HY-B0352S
    Mirtazapine-d3
    Inhibitor 98.55%
    Mirtazapine-d3 is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.
    Mirtazapine-d<sub>3</sub>
  • HY-107613A
    R 59-022 hydrochloride
    Antagonist 98.88%
    R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
    R 59-022 hydrochloride
  • HY-100943
    Cinanserin hydrochloride
    Antagonist 99.48%
    Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
    Cinanserin hydrochloride
  • HY-10560
    Temanogrel
    Antagonist 98.94%
    Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.
    Temanogrel
  • HY-B1737
    Pirenperone
    Antagonist 98.74%
    Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity.
    Pirenperone
  • HY-101367A
    GR 55562 dihydrochloride
    Antagonist ≥99.0%
    GR 55562 dihydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 dihydrochloride can be used for the research of nerve disease.
    GR 55562 dihydrochloride
  • HY-B0407AS
    Chlorpromazine-d6 hydrochloride
    99.88%
    Chlorpromazine-d6 (hydrochloride) is the deuterium labeled Chlorpromazine. Chlorpromazine is an inhibitor of dopamine receptor, 5-HT receptor, potassium channel, sodium channel.
    Chlorpromazine-d<sub>6</sub> hydrochloride
  • HY-124501
    LY 165163
    Agonist 99.24%
    LY 165163 is a potent 5-HT presynaptic receptor agonist. LY 165163 significantly decreases 5-HTP accumulation and increases DOPA accumulation in the cortex and striatum.
    LY 165163
  • HY-118152
    Org-12962
    Agonist 99.93%
    Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
    Org-12962
  • HY-15780S
    Brexpiprazole-d8
    Modulator ≥99.0%
    Brexpiprazole-d8 (OPC-34712-d8) 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>
  • HY-14539S2
    Clozapine-d4
    Modulator 99.82%
    Clozapine-d4 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>4</sub>
  • HY-128901
    F 13714 fumarate
    Agonist 99.05%
    F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress.
    F 13714 fumarate
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