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-110330
    R 1485 dihydrochloride
    		Antagonist
    R 1485 is a 5-HT6 receptor antagonist.
    R 1485 dihydrochloride
  • HY-103199
    Carpindolol
    		Modulator
    Carpindolol (SDZ21009) is a 5-HT1B receptor antagonist (pKd of 8.53 and pKB of 8.0) and a 5-HT1D receptor agonist (pEC50 of 5.91 and pKd of 6.37).
    Carpindolol
  • HY-118008A
    Lesopitron hydrochloride
    		Agonist
    Lesopitron hydrochloride is a 5-HT receptor agonist with potent anxiolytic-like effects. Lesopitron hydrochloride inhibits forskolin-stimulated adenylate cyclase activity with an IC50 value of 125 nM.
    Lesopitron hydrochloride
  • HY-103132
    PNU109291
    		Agonist
    PNU109291 is a potent and selective 5-HT1D agonist. PNU109291 reduces dural plasma extravasation evoked by trigeminal ganglion stimulation.
    PNU109291
  • HY-101377B
    S(-)-8-OH-DPAT hydrobromide
    		Agonist
    S(-)-8-OH-DPAT (S(-)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is an enantiomer of 8-OH-DPAT hydrobromide. 8-OH-DPAT hydrobromide is a potent, selective 5-HT1A agonist with a pIC50 of 8.19.
    S(-)-8-OH-DPAT hydrobromide
  • HY-182373
    5-HT2C agonist-13
    		Agonist
    5-HT2C agonist-13 is an orally active, selective and brain-penetrant 5-HT2C receptor agonist with human 5-HT2C receptor EC50 of 16 nM, Ki of 20 nM. 5-HT2C agonist-13 functionally activates 5-HT2C receptors, reduces food intake, reduces body weight gain, and exhibits effects reversible by a selective 5-HT2C antagonist. 5-HT2C agonist-13 can be used for the research of obesity.
    5-HT2C agonist-13
  • HY-146677
    5-HT6R/MAO-B modulator 1
    		Antagonist
    5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT6R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits. 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    5-HT6R/MAO-B modulator 1
  • HY-143797S
    Almotriptan-d6 maleate
    		Agonist
    Almotriptan-d6 (PNU180638-d6) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.
    Almotriptan-d<sub>6</sub> maleate
  • HY-B0965AR
    Thioridazine (Standard)
    		Antagonist
    Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine (Standard)
  • HY-117799C
    (±)-LY-426965 dihydrochloride
    		Control
    (±)-LY-426965 dihydrochloride is a racemate of LY-426965 (HY-117799). LY426965 is a potent 5-HT1A receptor antagonist.
    (±)-LY-426965 dihydrochloride
  • HY-179008A
    (S)-5-HT2CR agonist 1
    		Agonist
    (S)-5-HT2CR agonist 1 (Compound (S)-16k) is selective 5-HT2CR agonist, with an EC50 of 14 nM. FXa-IN-2 can be used in the research of hyperlocomotion.
    (S)-5-HT2CR agonist 1
  • HY-103144
    WAY 629 hydrochloride
    		Agonist
    WAY 629 hydrochloride is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 hydrochloride decreases feeding behavior.
    WAY 629 hydrochloride
  • HY-70050CR
    Alosetron Hydrochloride (Standard)
    		Antagonist
    Alosetron (Hydrochloride) (Standard) is the analytical standard of Alosetron (Hydrochloride). This product is intended for research and analytical applications. Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
    Alosetron Hydrochloride (Standard)
  • HY-113643
    Levemopamil hydrochloride
    		Antagonist
    Levemopamil hydrochloride is a blood-brain barrier penetrable calcium channel blocker and a 5-HT2 antagonist. Levemopamil hydrochloride can be used for temporary occlusion and neurological disease research.
    Levemopamil hydrochloride
  • HY-109118
    Masupirdine free base
    		Antagonist
    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease.
    Masupirdine free base
  • HY-13052
    SB-737050A
    		Antagonist
    SB-737050A is a potent 5-HT6 antagonist to prevent relapse into addiction.
    SB-737050A
  • HY-124367
    25B-NBF hydrochloride
    		Agonist
    25B-NBF hydrochloride is a highly potent agonist for the 5-HT2C receptor binds human 5-HT2A receptors and rat 5-HT2C receptors with pKi values of 8.57 and 7.73, respectively.
    25B-NBF hydrochloride
  • HY-181425
    N-Desmethyl xanomeline
    N-Desmethyl xanomeline is a pharmacologically active metabolite of Xanomeline (HY-105182). N-Desmethyl xanomeline binds to muscarinic, serotonergic, histaminergic and dopaminergic receptors. N-Desmethyl xanomeline can be used for the research of schizophrenia.
    N-Desmethyl xanomeline
  • HY-N1957R
    Gamma-Mangostin (Standard)
    		Antagonist
    Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes.
    Gamma-Mangostin (Standard)
  • HY-17382R
    Metoclopramide (Standard)
    		Antagonist
    Metoclopramide (Standard) is the analytical standard of Metoclopramide. This product is intended for research and analytical applications. Metoclopramide is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
    Metoclopramide (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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