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-155116
    5-HT6 agonist 1
    		Agonist
    5-HT6 agonist 1 (Compound 19) is a 5-HT6 agonist (Ki: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability.
    5-HT6 agonist 1
  • HY-18276
    SUVN-507
    		Antagonist
    SUVN-507 is a 5-HT6 receptor antagonist. SUVN-507 can reverse cognitive impairments and enhance excitatory neural transmission while weakening inhibitory neural transmission. SUVN-507 can be used for the research of neurological disease, such as Alzheimer's disease.
    SUVN-507
  • HY-15472A
    PRX-08066 maleate
    		Antagonist
    PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066 maleate
  • HY-111491
    Methiothepin
    		Antagonist
    Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
    Methiothepin
  • HY-169446
    ALEPH hydrochloride
    		Agonist
    ALEPH (hydrochloride) is the h5-HT2A and h5-HT2B partial agonist with the EC50 values of 10.3 nM and 19.2 nM, respectively. ALEPH (hydrochloride) causes head twitch response in mice (ED50: 0.80 mg/kg).
    ALEPH hydrochloride
  • HY-121001
    Amanozine
    		Agonist
    Amanozine (Compound 15) is a 5-HT3 serotonin receptor agonist. Amanozine is promising for research of nervous system disorders.
    Amanozine
  • HY-106465
    Proterguride
    		Agonist
    Proterguride is a potent dopamine receptor agonist. Proterguride also shows antagonistic properties at the histamine H(1) receptor and alpha(1)-adrenoceptor and partially agonize serotonergic 5-HT2A/B receptor. Proterguride can be used for the research of neurological disease, such as Parkinson's disease .
    Proterguride
  • HY-165624
    LY-41
    LY-41 is a 2-aminotetralin (HY-W022362) derivative related to 8-OH-DPAT (HY-112061). LY-41 decreases 5-HT synthesis. LY-41 induces 5-HT motor syndrome. (R)-LY-41 and (S)-LY-41 are novel 5-HT1A receptor agonists.
    LY-41
  • HY-103146
    GR125487 sulfamate
    		Antagonist
    GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction.
    GR125487 sulfamate
  • HY-101105
    SB-224289
    		Antagonist
    SB-224289 is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
    SB-224289
  • HY-107125A
    AVN-322 free base
    		Antagonist
    AVN-322 free base is an orally active, highly selective 5-HT6Rantagonist for central nervous system disease research.
    AVN-322 free base
  • HY-118836
    GSK215083
    		Antagonist
    GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation.
    GSK215083
  • HY-175816
    5-HT6R/FAAH modulator 1
    		Modulator
    5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pKi of 6.33 (5-HT6) and a pIC50 valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC50 = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).
    5-HT6R/FAAH modulator 1
  • HY-10351
    Robalzotan
    		Inhibitor
    Robalzotan (NAD-​299) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan increases the firing rate of 5-HT cells. Robalzotan induces 5-HT1A receptor occupancy. Robalzotan has the potential for the research of a cholinergic deficit in the central -nervous system.
    Robalzotan
  • HY-167663A
    (S)-Ebalzotan
    		Agonist
    (S)-Ebalzotan is the S-form of Ebalzotan (HY-167663). Ebalzotan is a 5-HT1A receptor agonist with activity in the study of depression. Ebalzotan can serve as a precursor to important active pharmaceutical ingredients. The synthesis of Ebalzotan involves a multi-enzyme catalyzed reduction reaction to obtain saturated primary or secondary alcohols in high yields and high enantioselectivity.
    (S)-Ebalzotan
  • HY-105449A
    KB R6933
    		Antagonist
    KB R6933 (KB 6806 maleate) is a potent, selective and orally active 5-HT3 receptor antagonist. KB R6933 can inhibit the diarrhea induced by 5-HT (HY-B1473A), but not that by Castor Oil (HY-107799) or prostaglandin E2 (PGE2) (HY-101952). KB R6933 can inhibit 5-HT-induced bradycardia.
    KB R6933
  • HY-46286
    TTFB
    		Control 99.83%
    TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn2+- and H+-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
    TTFB
  • HY-107626A
    ATC0065 free base
    ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities.
    ATC0065 free base
  • HY-107847
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
    		Agonist 99.65%
    2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
  • HY-106487
    Pridefine
    		Inhibitor
    Pridefine (AHR-1118) is an antidepressant agent.
    Pridefine
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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