1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101357
    CP 93129
    Agonist
    CP 93129 is a potent and selective 5-HT1B agonist. CP 93129 has the potential for the research of Parkinson's disease.
    CP 93129
  • HY-165440
    Cyclobenzaprine
    Antagonist
    Cyclobenzaprine (MK130) is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Cyclobenzaprine also possesses antiparasitic activity. Cyclobenzaprine holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases.
    Cyclobenzaprine
  • HY-108227
    Quetiapine sulfone
    Agonist
    Quetiapine sulfone is a main metabolite of Quetiapine (HY-14544). Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.
    Quetiapine sulfone
  • HY-17382S
    Metoclopramide-d3
    Antagonist
    Metoclopramide-d3 is deuterium labeled Metoclopramide. 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-d<sub>3</sub>
  • HY-121249
    Capeserod hydrochloride
    Agonist
    Capeserod hydrochloride (SL65.0155) is a 5-HT4(e) receptor partial agonist (Ki=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing 5-HT4(b) and 5-HT4(e) splice variants, stimulating cAMP production with IC50 values of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia.
    Capeserod hydrochloride
  • HY-W745430
    Cyproheptadine hydrochloride-d3
    Cyproheptadine hydrochloride-d3 (Cyproheptadine HCl-d3) is the deuterium labeled Cyproheptadine hydrochloride (HY-B0366A). Cyproheptadine hydrochloride is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders.
    Cyproheptadine hydrochloride-d<sub>3</sub>
  • HY-B2073A
    Clocapramine dihydrochloride hydrate
    Antagonist
    Clocapramine hydrochloride hydrate is an antagonist of the D2 and 5-HT2A receptors.
    Clocapramine dihydrochloride hydrate
  • HY-116524
    PF-04781340
    Agonist
    PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile.
    PF-04781340
  • HY-105704
    Danitracen
    Antagonist
    Danitracen (NSC 170955) is an orally active, CNS penetrant serotonin antagonist with antidepressant activity. Danitracen reduces serotonin levels in the cerebrum, cerebellum, medulla and the whole brain. Danitracen exhibits anticataleptic effects in rat catalepsy models. Danitracen can be used for catalepsy and depression research.
    Danitracen
  • HY-109067
    Opiranserin
    Antagonist
    Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
    Opiranserin
  • HY-136842
    Oxetorone fumarate
    Antagonist
    Oxetorone fumarate is a non-selective, orally active serotonin antagonist. Oxetorone fumarate is an antimigraine agent.
    Oxetorone fumarate
  • HY-148718
    4-Chloro Trazodone hydrochloride
    Control
    4-Chloro Trazodone hydrochloride is an isomer of Trazodone hydrochloride (HY-B0478). Trazodone hydrochloride is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
    4-Chloro Trazodone hydrochloride
  • HY-101630A
    Deramciclane fumarate
    Antagonist
    Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis.
    Deramciclane fumarate
  • HY-19733S1
    Lumateperone-d4 tosylate
    Antagonist
    Lumateperone-d4 tosylate (ITI-007-d4 tosylate) is the deuterium labeled Lumateperone tosylate (HY-19733). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
    Lumateperone-d<sub>4</sub> tosylate
  • HY-172980
    5-HT2A receptor agonist-9
    Agonist
    5-HT2A receptor agonist-9 (Compound 9) is a β-arrestin-biased 5-HT2A receptor agonist. 5-HT2A receptor agonist-9 can be used in the research of neurological diseases such as antidepressant and psychedelic.
    5-HT2A receptor agonist-9
  • HY-21995
    BGC20-761
    Antagonist
    BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor Ki values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent.
    BGC20-761
  • HY-177314
    5-HT1A antagonist 2
    Antagonist
    5-HT1A antagonist 2 (example 1) is a 5-HT1A antagonist that can be used to study depression or attention deficit hyperactivity disorder (ADHD).
    5-HT1A antagonist 2
  • HY-W016194R
    1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard)
    1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) is the analytical standard of 1-(Carboxymethyl)cyclohexanecarboxylic acid. This product is intended for research and analytical applications. 1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
    1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard)
  • HY-125973
    S(-)-Cyanopindolol hemifumarate
    Antagonist
    S(−)-Cyanopindolol hemifumarate is an isomer of Cyanopindolol (HY-W795507). S(-)-Cyanopindolol hemifumarate is a 5-HT1A/1B serotonin receptor antagonist and a β3-adrenoceptor antagonist.
    S(-)-Cyanopindolol hemifumarate
  • HY-106484
    Tiflucarbine
    Agonist
    Tiflucarbine (BAY-P 4495) is a tetrahydrothieno-7-carboline derivative. Tiflucarbine is a potent antidepressant agent that binds at central serotonin (5-HT) binding sites. Tiflucarbine is a nonselective 5-HT (5-HT1 and 5-HT2) agonist.
    Tiflucarbine
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