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
(455)
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5-HT2 Receptor
(490)
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5-HT3 Receptor
(34)
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5-HT4 Receptor
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5-HT5 Receptor
(14)
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5-HT6 Receptor
(86)
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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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Productos relacionados con 5-HT Receptor (1771)
Productos relacionados con (1771)
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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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NAS-181 dimesylate
0 ImagesReferencia número: HY-103156No. CAS: 1217474-40-2NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
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Lumateperone tosylate
0 ImagesSynonyms: ITI-007 tosylateLumateperone (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.
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Tropisetron
0 ImagesSynonyms: SDZ-ICS-930 free baseTropisetron is an orally active 5-HT3R antagonist (Ki = 5.3 nM) as well as being a potent and selective α7 nicotinic partial agonist (EC50 = 1.3 μM). Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion.
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Mosapride citrate dihydrate
0 ImagesSynonyms: TAK-370 citrate dihydrate; AS-4370 citrate dihydrateMosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.
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Talipexole dihydrochloride
0 ImagesSynonyms: B-HT 920 dihydrochlorideTalipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
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SB 258719
0 ImagesSB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease.
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JNJ-18038683
0 ImagesJNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
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Vabicaserin hydrochloride
0 ImagesSynonyms: SCA-136Vabicaserin hydrochloride (SCA-136) is a brain-penetrant, orally active, and selective 5-HT2C receptor agonist (Ki = 3 nM; EC50 = 8 nM). Vabicaserin hydrochloride specifically activates Gq-coupled 5-HT2C receptors to promote calcium mobilization, thereby selectively reducing dopamine release in the mesolimbic system without affecting the nigrostriatal pathway. Vabicaserin hydrochloride is an antagonist of 5-HT2A/5-HT2B receptors. Vabicaserin hydrochloride can be used for research on schizophrenia, obesity, chronic pain, and neurodegenerative diseases (such as Machado-Joseph disease).
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BRL 54443
0 ImagesBRL 54443 is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.
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Viloxazine
0 ImagesSynonyms: Viloxazin; EmovitViloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD).
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SB 271046 Hydrochloride
0 ImagesSynonyms: SB 271046ASB 271046 Hydrochloride (SB 271046A) is a potent, selective, orally active and BBB-permeable 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).
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GR127935 hydrochloride
0 ImagesGR127935 hydrochloride is a selective and orally active 5-HT1D and 5-HT1B receptor antagonist with pKi values of 8.5 for both receptors. GR127935 hydrochloride impairs memory acquisition and Serotonin (HY-B1473A)-mediated vasodilation. GR127935 hydrochloride can be used for research on amnesia, neuroendocrine cancer, and migraine.
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Lurasidone Hydrochloride
0 ImagesSynonyms: SM-13496 HydrochlorideLurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
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Setiptiline
0 ImagesSynonyms: Org-8282Setiptiline (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.
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Levosulpiride
0 ImagesSynonyms: RV-12309; S-(-)-SulpirideLevosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class.
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Azasetron hydrochloride
0 ImagesSynonyms: Y-25130 hydrochlorideAzasetron (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).
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uPSEM792
0 ImagesuPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM4-GlyR.
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Norquetiapine
0 ImagesSynonyms: N-DesalkylquetiapineNorquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.
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13,14-Dihydro-15-keto-PGE2
0 Images13,14-Dihydro-15-keto-PGE2 participates in Bifidobacterium animalis F1-7 to alleviate opioid-induced constipation by 5-HT pathway.
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Paliperidone palmitate
0 ImagesSynonyms: 9-Hydroxyrisperidone palmitatePaliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia.
