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.
5-HT Receptor Isoform Specific Products
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5-HT Receptor
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5-HT1 Receptor
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5-HT2 Receptor
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5-HT3 Receptor
(34)
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5-HT4 Receptor
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5-HT5 Receptor
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5-HT6 Receptor
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5-HT7 Receptor
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All Product Categories
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5-HT Receptor Inhibitors
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5-HT Receptor Agonists
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5-HT Receptor Antagonists
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5-HT Receptor Activators
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5-HT Receptor Modulators
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5-HT Receptor Inducers
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5-HT Receptor Controls
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5-HT Receptor Ligands
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5-HT Receptor Related Products (1763)
Related Products (1763)
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Antibodies (1)
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Related Compound Screening Libraries (1)
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5-HT Receptor Isoform Comparison
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SB 258741
0 ImagesCat. No.: HY-136678CAS No.: 201038-58-6SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.5) antagonist.
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5-HT6/5-HT2A receptor ligand-2
0 ImagesCat. No.: HY-146077CAS No.: 2411088-16-75-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.
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Flumezapine-d8 hydrochloride
0 ImagesCat. No.: HY-106605SSynonyms: LY 120363-d8 hydrochlorideFlumezapine-d8 (LY 120363-d8) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.
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5-HT6R antagonist 5
0 ImagesCat. No.: HY-171052CAS No.: 1220645-15-75-HT6R antagonist 5 (compound 1.2.12(4)) is a potent competitive 5-HT6R antagonist with an IC50 of 4.19 nM. 5-HT6R antagonist 5 can be used for research in various central nervous system (CNS) diseases, cognitive and neurodegenerative diseases.
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Indisetron dihydrochloride
0 ImagesCat. No.: HY-109543ACAS No.: 160472-97-9Indisetron dihydrochloride is a 5-HT3 receptor antagonist with anti-emetic activity.
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HTR2A antagonist 1
0 ImagesCat. No.: HY-168443HTR2A antagonist 1 (Compound 15f) is a HTR2A antagonist, with an IC50 of 42.79 nM. HTR2A antagonist 1 induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells via the activation of p53/p21/caspase 3 signaling. HTR2A antagonist 1 has good liver microsomal stability. HTR2A antagonist 1 can be used for the research of colorectal cancer.
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Cerlapirdine hydrochloride
0 ImagesCat. No.: HY-14431ACAS No.: 925447-04-7Synonyms: SAM-531 hydrochloride; PF-05212365 hydrochlorideCerlapirdine hydrochloride is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine hydrochloride has the potential for researching the Alzheimer's disease.
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5-HT3 antagonist-7
0 ImagesCat. No.: HY-182701CAS No.: 149685-89-25-HT3 antagonist-7 (Compound 7e) is a competitive and selective 5-HT3 receptor antagonist. 5-HT3 antagonist-7 inhibits 5-HT-induced contractions in guinea pig ileum and guinea pig thoracic aorta. 5-HT3 antagonist-7 prevents 2-methyl-5-HT-induced vomiting episodes in ferrets.
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SB-215505
0 ImagesSB-215505 is an orally active and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
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PNU-96415E
0 ImagesCat. No.: HY-103404CAS No.: 170856-41-4PNU-96415E is a selective D4/5-HT2A antagonist. PNU-96415E may have potential antipsychotic efficacy.
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Octoclothepin dimaleate
0 ImagesCat. No.: HY-106587BCAS No.: 41932-42-7Synonyms: Clorotepine dimaleateOctoclothepin (Clorotepine) dimaleate is a D2 dopamine receptor antagonist and 5-HT2 serotonin receptor antagonist , with Ki values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D2, 5-HT2A, and 5-HT2C receptors, respectively. Octoclothepin dimaleate also binds to adrenergic receptors, with Ki values of 0.66 nM, 0.56 nM, and 0.77 nM for α1a, α1b, and α1d, respectively. Octoclothepin dimaleate can be used in schizophrenia research.
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PNU-282987 free base
0 ImagesCat. No.: HY-12560CAS No.: 711085-63-1PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems.
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Amesergide
0 ImagesCat. No.: HY-105277CAS No.: 121588-75-8Amesergide is a serotonin (5-HT1C/2) antagonist. Amesergide can result in a reduction of progeny body weight gains in maternal animals. Amesergide can be studied in research on depression.
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LY-426965
0 ImagesCat. No.: HY-117799CAS No.: 228418-82-4LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders.
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5-HT6/5-HT2A receptor ligand-1
0 ImagesCat. No.: HY-146076CAS No.: 2411088-07-65-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research.
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SB 714786
0 ImagesCat. No.: HY-121562CAS No.: 584555-10-2SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.
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Mirtazapine-d4 hydrochloride
0 ImagesCat. No.: HY-B0352S3CAS No.: 1215587-73-7Mirtazapine-d4 hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
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Pelanserin
0 ImagesPelanserin (Compound 1) is an orally active antihypertensive agent. Pelanserin is a potent 5-HT2 receptor antagonist. Pelanserin has the ability to block the activity of α-adrenergic receptor, with its ED50 being 0.03 μg/mL. Pelanserin has vasodilatory activity, with its ED100 being 5 μg. Pelanserin exhibits antihypertensive activity in hypertensive rats and renal hypertensive dog breeds. Pelanserin can be used for research on hypertension.
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Tenilapine
0 ImagesCat. No.: HY-155215CAS No.: 82650-83-7Tenilapine displays potent inverse agonist activity at rat and human 5-HT(2C) receptors.
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Pellotine
0 ImagesCat. No.: HY-170908CAS No.: 19622-05-0Pellotine is an alkaloid that can be isolated from Lophophora. Pellotine is the inverse agonist for 5-HT7 receptor with an EC50 of 291 nM. Pellotine exhibits good affinity to 5-HT1DR and 5-HT6R with Ki of 117 nM and 170 nM. Pellotine reduces intracellular cAMP levels, thereby reducing neuronal excitability and neurotransmitter release.
