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-13409R
    SB 242084 (Standard)
    		Antagonist
    SB 242084 (Standard) is the analytical standard of SB 242084. This product is intended for research and analytical applications. SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.
    SB 242084 (Standard)
  • HY-103108R
    CJ033466 (Standard)
    		Agonist
    CJ033466 (Standard) is the analytical standard of CJ033466 (HY-103108). This product is intended for research and analytical applications. CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect.
    CJ033466 (Standard)
  • HY-32329R
    Setiptiline (Standard)
    		Modulator
    Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
    Setiptiline (Standard)
  • HY-15543
    CP-809101
    		Agonist
    CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.
    CP-809101
  • HY-19682
    Enciprazine
    		Agonist
    Enciprazine is an orally active non-benzodiazepine anxiolytic. Enciprazine acts as an agonist of 5-HT1A receptor (5-HT1AR) and an antagonist of α1-adrenergic receptor (α1-adrenergic receptor) . Enciprazine induces drug-related electroencephalogram changes by reducing the average power of δ waves and θ waves, and increasing the average power of α waves and fast β waves. Enciprazine exhibits anti-aggressive activity, with only weak sedative and ataxic effects. Enciprazine regulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis. Enciprazine can be used in research related to anxiety disorders, generalized anxiety syndrome and psychosis.
    Enciprazine
  • HY-101365AR
    RS-102221 hydrochloride (Standard)
    		Antagonist
    RS-102221 (hydrochloride) (Standard) is the analytical standard of RS-102221 (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-19283
    DU125530
    		Antagonist
    DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects.
    DU125530
  • HY-103130R
    EMD386088 (Standard)
    		Agonist
    EMD386088 (Standard) is the analytical standard of EMD386088 (HY-103130). This product is intended for research and analytical applications. EMD386088 is a potent and selective 5-HT6 receptor (5-HT6R) agonist with an EC50 of 1.0 nM. EMD-386088 is inactive against other HT receptors except 5-HT3R (IC50 of 34 nM). EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.
    EMD386088 (Standard)
  • HY-108256S
    Melitracen-d6 hydrochloride
    		Inhibitor
    Melitracen-d6 (hydrochloride) is the deuterium labeled Melitracen hydrochloride. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
    Melitracen-d<sub>6</sub> hydrochloride
  • HY-100942R
    5-Carboxamidotryptamine maleate (Standard)
    		Agonist
    5-Carboxamidotryptamine (maleate) (Standard) is the analytical standard of 5-Carboxamidotryptamine (maleate) (HY-100942). This product is intended for research and analytical applications. 5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptors agonist.
    5-Carboxamidotryptamine maleate (Standard)
  • HY-W181626A
    Tiprenolol hydrochloride
    		Inhibitor
    Tiprenolol hydrochloride is a β-adrenoceptor blocker. Tiprenolol hydrochloride abolished ventricular arrhythmias induced by intravenous epinephrine in dogs receiving halothane inhalation.
    Tiprenolol hydrochloride
  • HY-100554R
    BMY 7378 (Standard)
    		Agonist
    BMY 7378 (Standard) is the analytical standard of BMY 7378 (HY-100554). This product is intended for research and analytical applications. BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
    BMY 7378 (Standard)
  • HY-14558R
    Tandospirone (Standard)
    		Agonist
    Tandospirone (Standard) is the analytical standard of Tandospirone. This product is intended for research and analytical applications. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.
    Tandospirone (Standard)
  • HY-101638A
    (±)-Fabesetron
    		Antagonist
    (±)-Fabesetron ((±)-FK1052 free base) is the racemate of Fabesetron, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
    (±)-Fabesetron
  • HY-U00322
    5-HT3 antagonist 3
    		Antagonist
    5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with Ki of 0.25 nM.
    5-HT3 antagonist 3
  • HY-U00234
    Zatosetron maleate
    		Antagonist
    Zatosetron maleate is a potent and selective 5HT3 receptor antagonist.
    Zatosetron maleate
  • HY-U00356
    Tertatolol
    		Antagonist
    Tertatolol is a potent antagonist of beta-adrenoceptor and 5-HT receptor, with unique renal vasodilatatory effects.
    Tertatolol
  • HY-U00367
    (4E)-SUN9221
    		Antagonist
    (4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.
    (4E)-SUN9221
  • HY-U00368
    5-HT3 antagonist 1
    		Antagonist
    5-HT3 antagonist 1 is a potent and selective antagonist of serotonin 3 (5-HT3) receptor.
    5-HT3 antagonist 1
  • HY-U00413
    5-HT3-In-1
    		Inhibitor
    5-HT3-In-1 is extracted from patent EP0748807A1, compound example 8. It shows 5-HT3 inhibition activity.
    5-HT3-In-1
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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