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-B0383R
    Almotriptan malate (Standard)
    		Agonist
    Almotriptan (malate) (Standard) is the analytical standard of Almotriptan (malate). This product is intended for research and analytical applications.
    Almotriptan malate (Standard)
  • HY-B0121BS3
    Sumatriptan-d6 formate
    		Agonist
    Sumatriptan-d6 (formate) (GR 43175 free base-d6 (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research.
    Sumatriptan-d<sub>6</sub> formate
  • HY-175192
    5-HT2A agonist 5
    		Agonist
    5-HT2A agonist 5 (Compound 88) is a 5-HT2A agonist with an EC50 of 0.01  nM for h5-HT2A. 5-HT2A agonist 5 can be used for depression, drug addiction, alcoholism, post-traumatic stress disorder (PTSD), and neuropathic pain research.
    5-HT2A agonist 5
  • HY-108173
    TKS 159
    		Agonist
    TKS 159 is a 5-HT4 receptor agonist. TKS 159 can promote gastrointestinal motility. TKS 159 can be used for research on gastrointestinal conditions.
    TKS 159
  • HY-135021
    3,4-Dihydro Naratriptan
    		Agonist
    3,4-Dihydro Naratriptan is a serotonin 5-HT1-receptor agonist. 3,4-Dihydro Naratriptan exhibits selective vasoconstrictor activity. 3,4-Dihydro Naratriptan can be used for migraine diseases research.
    3,4-Dihydro Naratriptan
  • HY-B0197AR
    Naratriptan hydrochloride (Standard)
    		Agonist
    Naratriptan (GR-85548A) hydrochloride (Standard) is the analytical standard of Naratriptan hydrochloride (HY-B0197A). This product is intended for research and analytical applications. Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
    Naratriptan hydrochloride (Standard)
  • HY-13788B
    LY 344864 hydrochloride
    		Agonist
    LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent.
    LY 344864 hydrochloride
  • HY-179713
    D2R/D3R/5-HT1AR agonist 1
    		Agonist
    D2R/D3R/5-HT1AR agonist 1 (compound 22b) is an orally active triple-target D2R/D3R/5-HT1AR agonist with EC50 values of 1.29, 1.05 and 153.5 nM. D2R/D3R/5-HT1AR agonist 1 can improve the behavioral disorders induced by MPTP (HY-W114750) and exerts anti-depression effect. D2R/D3R/5-HT1AR agonist 1 can be used for the research of Parkinson's disease and depression.
    D2R/D3R/5-HT1AR agonist 1
  • HY-179684
    PCC0105005
    		Agonist
    PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine.
    PCC0105005
  • HY-170053
    4-Hydroxy MPT
    		Agonist
    4-Hydroxy MPT (4-OH-MPT), a serotonergic hallucinogen, is a 5-HT2A and 5-HT2B receptors agonist with EC50 values of 3.82 nM and 3.4 nM, respectively.
    4-Hydroxy MPT
  • HY-106385
    PRX-03140
    		Agonist
    PRX-03140 is a selective, blood-brain-barrier permeable 5-HT4 receptor agonist with a Ki value of 110 nM against rat brain 5-HT4 receptor. PRX-03140 can increase cortical ACh and histamine levels. PRX-03140 can be used in the research of Alzheimer's disease.
    PRX-03140
  • HY-15394S
    (Rac)-Rotigotine-d7 (hydrochloride)
    		Agonist
    (Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine-d<sub>7</sub> (hydrochloride)
  • HY-103091
    Donitriptan hydrochloride
    		Agonist
    Donitriptan hydrochloride (F-11356) is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
    Donitriptan hydrochloride
  • HY-145698
    UCSF678
    		Agonist
    UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR.
    UCSF678
  • HY-B0206S
    Rizatriptan-d6 benzoate
    		Agonist
    Rizatriptan-d6 (benzoate) is the deuterium labeled Rizatriptan benzoate. Rizatriptan benzoate is the agonist for 5-HT1B and 5-HT1D. Rizatriptan benzoate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system.
    Rizatriptan-d<sub>6</sub> benzoate
  • HY-101049
    CGS 12066 dimaleate
    		Agonist
    CGS 12066 (dimaleate) dimaleate is a selective 5-HT1B receptor agonist with an IC50 of 51 nM.
    CGS 12066 dimaleate
  • HY-W018475
    Rizatriptan
    		Agonist
    Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache.
    Rizatriptan
  • HY-B0121A
    Sumatriptan hydrochloride
    		Agonist
    Sumatriptan hydrochloride (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan hydrochloride can be used for migraine headache research.
    Sumatriptan hydrochloride
  • HY-21994
    Org-12962 hydrochloride
    		Agonist
    Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.
    Org-12962 hydrochloride
  • HY-103144A
    WAY 629
    		Agonist
    WAY 629 is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 decreases feeding behavior.
    WAY 629
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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