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-B0068
    Azasetron hydrochloride
    		Antagonist 99.76%
    Azasetron (Y-25130) hydrochloride, a benzamide derivative, is a potent and selective 5-HT3 receptor antagonist. Azasetron is used in the study for Chemotherapy-induced nausea and vomiting (CINV).
    Azasetron hydrochloride
  • HY-103101
    LP44 hydrochloride
    		Agonist 98.06%
    LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration.
    LP44 hydrochloride
  • HY-N0749A
    Jatrorrhizine hydroxide
    		Inhibitor 98.07%
    Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
    Jatrorrhizine hydroxide
  • HY-109112
    Brilaroxazine
    		Modulator 98.29%
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
    Brilaroxazine
  • HY-125784
    Viloxazine hydrochloride
    		Inhibitor 98.94%
    Viloxazine hydrochloride is the hydrochloride salt form of Viloxazine (HY-W380450). Viloxazine (Viloxazin) hydrochloride is a norepinephrine reuptake inhibitor and a potent 5-HT2C agonist agent and 5-HT2B antagonist, EC50 for 5-HT2C b> is 32 μM, and the IC50 for 5-HT2B is 27 μM. Viloxazine hydrochloride's mechanism of action primarily involves serotonergic and noradrenergic pathways. Viloxazine hydrochloride is used in antidepressant research.
    Viloxazine hydrochloride
  • HY-19818A
    NAN-190 hydrobromide
    		Antagonist 99.11%
    NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A.
    NAN-190 hydrobromide
  • HY-107613A
    R 59-022 hydrochloride
    		Antagonist 98.88%
    R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
    R 59-022 hydrochloride
  • HY-101094
    Ocaperidone
    		Modulator 99.93%
    Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
    Ocaperidone
  • HY-17038A
    Agomelatine hydrochloride
    		Antagonist 99.98%
    Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
    Agomelatine hydrochloride
  • HY-B0115
    Pizotifen
    		Antagonist 98.40%
    Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen
  • HY-10457
    Velusetrag
    		Agonist 99.91%
    Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease.
    Velusetrag
  • HY-B0197A
    Naratriptan hydrochloride
    		Agonist 99.91%
    Naratriptan hydrochloride is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.
    Naratriptan hydrochloride
  • HY-101324A
    MK-212 monohydrochloride
    		Agonist 99.62%
    MK-212 (CPP) monohydrochloride is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 monohydrochloride can stimulate phosphoinositide hydrolysis in cerebral cortex.
    MK-212 monohydrochloride
  • HY-B1107
    Naftidrofuryl oxalate
    		Antagonist 98.39%
    Naftidrofuryl oxalate (Nafronyl oxalate salt) is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.
    Naftidrofuryl oxalate
  • HY-101341
    RS 67333 hydrochloride
    		Agonist 99.73%
    RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.
    RS 67333 hydrochloride
  • HY-100562
    Flopropione
    		Antagonist 98.57%
    Flopropione is a 5-HT receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Flopropione also as an antispasmodic agent.
    Flopropione
  • HY-101222
    SB-203186 hydrochloride
    		Antagonist 99.94%
    SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
    SB-203186 hydrochloride
  • HY-117083
    Clothiapine
    		Antagonist 99.93%
    Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties.
    Clothiapine
  • HY-20696
    Tetrahydro-β-carboline
    		Inhibitor
    Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 µM.
    Tetrahydro-β-carboline
  • HY-14336A
    SB 271046 Hydrochloride
    		Antagonist 99.93%
    SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
    SB 271046 Hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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