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-106157
    Donitriptan
    		Agonist 98.06%
    Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
    Donitriptan
  • HY-100794
    GR127935 hydrochloride
    		Antagonist 99.38%
    GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research.
    GR127935 hydrochloride
  • HY-133152S
    Brexpiprazole S-oxide-d8
    		Modulator 98.72%
    Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine 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[1][2][3].
    Brexpiprazole S-oxide-d<sub>8</sub>
  • HY-16687A
    Eltoprazine hydrochloride
    		Modulator 99.90%
    Eltoprazine (DU 28853) hydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine hydrochloride shows antiaggressive and anxiogenic effects.
    Eltoprazine hydrochloride
  • HY-153912
    5-HT2A receptor agonist-3
    		Agonist 98.53%
    5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor.
    5-HT2A receptor agonist-3
  • HY-90003
    Tianeptine
    		Agonist 99.84%
    Tianeptine is a selective facilitator of 5-HT uptake. Tianeptine 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 has antidepressant, anxiolytic, analgesic and neuroprotective activities.
    Tianeptine
  • HY-121301
    Amperozide
    		Antagonist 98.75%
    Amperozide is an atypical antipsychotic that acts as an antagonist of the 5-HT2 receptor with a Ki value of 26 nM. Amperozide has a low affinity for D2 receptors.
    Amperozide
  • HY-14338A
    Idalopirdine hydrochloride
    		Antagonist 99.96%
    Idalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
    Idalopirdine hydrochloride
  • 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[1][2].
    Olanzapine-d<sub>3</sub>
  • HY-100703
    Pipamperone
    		Antagonist 99.89%
    Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7).
    Pipamperone
  • HY-101046
    Azaperone dimaleate
    		Agonist 99.87%
    Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research.
    Azaperone dimaleate
  • HY-100656
    Desmethyl cariprazine
    		Modulator 98.06%
    Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic agent candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).
    Desmethyl cariprazine
  • HY-100851A
    LY-272015 hydrochloride
    		Antagonist 99.54%
    LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
    LY-272015 hydrochloride
  • HY-14539R
    Clozapine (Standard)
    		Modulator 99.98%
    Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine (Standard)
  • HY-103094
    LY266097 hydrochloride
    		Inhibitor 99.60%
    LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.
    LY266097 hydrochloride
  • HY-119156
    Altanserin
    		99.93%
    Altanserin can synthesize Fluorine-18 Altanserin. Fluorine-18 Altanserin binds to the brain 5HT2 receptors.
    Altanserin
  • HY-B1101A
    Pimethixene maleate
    		Antagonist 99.94%
    Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
    Pimethixene maleate
  • HY-108509
    BMY-14802 hydrochloride
    		Agonist 98.02%
    BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.
    BMY-14802 hydrochloride
  • HY-100971
    Spiramide
    		Antagonist 99.23%
    Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity.
    Spiramide
  • HY-101172
    RS 23597-190
    		Antagonist 99.06%
    RS 23597-190 (EP-A-501322) is a high affinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits 5-HT (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose.
    RS 23597-190
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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