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Isoforms Recommended: 5-HT4 Receptor Apolipoprotein D
Results for "

5-HT4 Receptor

" in MedChemExpress (MCE) Product Catalog:

95

Inhibitors & Agonists

5

Natural
Products

6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14149
    Cisapride
    2 Publications Verification

    R 51619; (±)-Cisaprid

    5-HT Receptor Potassium Channel Neurological Disease
    Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .
    Cisapride
  • HY-B2132
    Tryptamine
    1 Publications Verification

    3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine

    Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor Neurological Disease Metabolic Disease
    Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .
    Tryptamine
  • HY-14151
    Prucalopride
    4 Publications Verification

    5-HT Receptor Apoptosis Autophagy Neurological Disease Cancer
    Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
    Prucalopride
  • HY-103152
    GR 113808
    Maximum Cited Publications
    9 Publications Verification

    5-HT Receptor Neurological Disease Inflammation/Immunology
    GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors .
    GR 113808
  • HY-12694
    Prucalopride succinate
    4 Publications Verification

    R-108512

    5-HT Receptor Apoptosis Autophagy Metabolic Disease Cancer
    Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
    Prucalopride succinate
  • HY-14153
    Tegaserod
    4 Publications Verification

    5-HT Receptor Apoptosis Metabolic Disease Cancer
    Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
    Tegaserod
  • HY-14153A
    Tegaserod maleate
    4 Publications Verification

    SDZ-HTF-919; HTF-919

    5-HT Receptor Apoptosis Neurological Disease Metabolic Disease Cancer
    Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
    Tegaserod maleate
  • HY-W015169

    O-Methylserotonin

    Drug Metabolite 5-HT Receptor Endogenous Metabolite Neurological Disease Cancer
    5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .
    5-Methoxytryptamine
  • HY-10564
    Sarpogrelate hydrochloride
    1 Publications Verification

    MCI-9042

    5-HT Receptor Cardiovascular Disease
    Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
    Sarpogrelate hydrochloride
  • HY-101341
    RS 67333 hydrochloride
    1 Publications Verification

    5-HT Receptor Neurological Disease
    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-15574
    Piboserod
    4 Publications Verification

    SB-207266

    5-HT Receptor Cardiovascular Disease
    Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .
    Piboserod
  • HY-10457

    TD-5108

    5-HT Receptor Neurological Disease Metabolic Disease
    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-101172

    EP-A-501322

    5-HT Receptor Cardiovascular Disease
    RS 23597-190 (EP-A-501322) is a high affinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits Serotonin (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .
    RS 23597-190
  • HY-116565
    Usmarapride
    1 Publications Verification

    SUVN-D4010

    5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) (Example 3)is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=27.5 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
    Usmarapride
  • HY-18137

    5-HT Receptor Neurological Disease
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
    PF-04995274
  • HY-B2089

    5-HT Receptor Dopamine Receptor Neurological Disease Metabolic Disease
    Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .
    Cinitapride
  • HY-134807

    P2X Receptor 5-HT Receptor Autophagy Cancer
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
    Indophagolin
  • HY-W015169A

    5-HT Receptor Endogenous Metabolite Neurological Disease Cancer
    5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .
    5-Methoxytryptamine hydrochloride
  • HY-110094
    BIMU 8
    1 Publications Verification

    5-HT Receptor Neurological Disease
    BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors .
    BIMU 8
  • HY-103137
    Zacopride hydrochloride
    1 Publications Verification

    5-HT Receptor Cardiovascular Disease Neurological Disease
    Zacopride hydrochloride is an orally active 5-HT3 receptor (Ki of 0.38 nM) antagonist and 5-HT4 receptor (Ki of 373 nM) agonist. Zacopride hydrochloride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride hydrochloride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety .
    Zacopride hydrochloride
  • HY-121826

    ATI-7505

    5-HT Receptor Metabolic Disease Inflammation/Immunology
    Naronapride (ATI-7505) is a potent prokinetic 5-HT4 receptor agonist. Naronapride can be used for gastrointestinal diseases research .
    Naronapride
  • HY-101222

    5-HT Receptor Cardiovascular Disease Neurological Disease
    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-10457A

    TD-5108 hydrochloride

    5-HT Receptor Neurological Disease Metabolic Disease
    Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
    Velusetrag hydrochloride
  • HY-100170

    5-HT Receptor Neurological Disease
    5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
    5-HT4 antagonist 1
  • HY-101668

    RS-100302

    5-HT Receptor Cardiovascular Disease
    Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
    Sulamserod
  • HY-103108

    5-HT Receptor Metabolic Disease
    CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect .
    CJ033466
  • HY-U00373
    Revexepride
    1 Publications Verification

    5-HT Receptor Cytochrome P450 Neurological Disease
    Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.
    Revexepride
  • HY-135439

    5-HT Receptor Neurological Disease
    SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .
    SB-203186
  • HY-14147

    BRL 24924

    5-HT Receptor Metabolic Disease
    Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist . Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study .
    Renzapride
  • HY-B2089R

    Reference Standards 5-HT Receptor Dopamine Receptor Neurological Disease Metabolic Disease
    Cinitapride (Standard) is the analytical standard of Cinitapride. This product is intended for research and analytical applications. Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .
    Cinitapride (Standard)
  • HY-15574A

    SB-207266 hydrochloride

    5-HT Receptor Cardiovascular Disease
    Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.
    Piboserod hydrochloride
  • HY-102057
    Felcisetrag
    1 Publications Verification

    TD-8954

    5-HT Receptor Others
    Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
    Felcisetrag
  • HY-14442

    5-HT Receptor Neurological Disease Metabolic Disease
    ML 10302 hydrochloride is a potent and selective 5-HT4 receptor agonist, with an EC50 of 4 nM. ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT3 receptor in binding assay .
    ML 10302 hydrochloride
  • HY-105201

    FK1052 free base

    5-HT Receptor Neurological Disease Cancer
    Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .
    Fabesetron
  • HY-116565A
    Usmarapride free base
    1 Publications Verification

    SUVN-D4010 free base

    5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .
    Usmarapride free base
  • HY-14149A
    Cisapride monohydrate
    2 Publications Verification

    R 51619 monohydrate; (±)-Cisaprid monohydrate

    5-HT Receptor Neurological Disease Metabolic Disease
    Cisapride monohydrate is an orally and potent 5-HT4 receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .
    Cisapride monohydrate
  • HY-10564R

    MCI-9042 (Standard)

    Reference Standards 5-HT Receptor Cardiovascular Disease
    Sarpogrelate (hydrochloride) (Standard) is the analytical standard of Sarpogrelate (hydrochloride). This product is intended for research and analytical applications. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
    Sarpogrelate hydrochloride (Standard)
  • HY-W822786

    5-HT Receptor Neurological Disease
    GR125487 is a highly selective and potent 5-HT4 receptor (5-HT4 receptor) antagonist with a Kd value of 0.1 nM. GR125487 has an extremely low affinity for 5-HT3 receptors (Kd > 1 μM). GR125487 completely antagonizes the memory-promoting effect of BIMU1, and its administration alone has no significant effect on basic social memory. GR125487 can be used for the study of social olfactory memory .
    GR125487
  • HY-12694R

    R-108512 (Standard)

    5-HT Receptor Apoptosis Autophagy Reference Standards Metabolic Disease Cancer
    Prucalopride (succinate) (Standard) is the analytical standard of Prucalopride (succinate). This product is intended for research and analytical applications. Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
    Prucalopride succinate (Standard)
  • HY-103134

    5-HT Receptor Inflammation/Immunology
    5-HT4 antagonist 3 hydrochloride is a highly selective 5-hydroxytryptamine receptor (5-HT4) antagonist. 5-HT4 antagonist 3 (hydrochloride) blocks muscarine receptors and sodium channels. 5-HT4 antagonist 3 (hydrochloride) can be used to evaluate function of 5-HT4 receptor .
    SB 204070A
  • HY-15574R

    SB-207266 (Standard)

    5-HT Receptor Reference Standards Cardiovascular Disease
    Piboserod (Standard) is the analytical standard of Piboserod. This product is intended for research and analytical applications. Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .
    Piboserod (Standard)
  • HY-101342

    5-HT Receptor Neurological Disease
    RS 67506 hydrochloride is a 5-HT4 receptor agonist. The pKi value of RS 67506 hydrochloride for 5-HT4 in guinea pig striatum is 8.8. RS 67506 hydrochloride can be used in neuro-related research .
    RS 67506 hydrochloride
  • HY-123747A

    5-HT Receptor Neurological Disease
    SC-53116 hydrochloride is a selective 5-HT4 receptor agonist with EC50 at 23 nM .
    SC-53116 hydrochloride
  • HY-123747

    5-HT Receptor Neurological Disease
    SC-53116 is a selective 5-HT4 receptor agonist with EC50 at 23 nM .
    SC-53116
  • HY-19927A

    5-HT Receptor Neurological Disease Endocrinology
    DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
    DA-6886 monohydrochloride
  • HY-109065

    5-HT Receptor Others
    Minesapride is a partial agonist with a highly selective serotonin 4 (5-HT4) receptor. Minesapride enhances gastrointestinal peristalsis and colon transport by activating the 5-HT4 receptor. Minesapride increases bowel movements and suppresses visceral allergic reactions. Minesapride can be used in the study of constipation-type irritable bowel syndrome (IBS-C) .
    Minesapride
  • HY-101668A

    RS-100302 hydrochloride

    5-HT Receptor Inflammation/Immunology
    Sulamserod hydrochloride is a 5-HT4 receptor antagonist. Sulamserod hydrochloride can be used in gastrointestinal disease related research .
    Sulamserod hydrochloride
  • HY-14441

    5-HT Receptor Neurological Disease
    ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases .
    ML 10302
  • HY-16729

    YKP10811

    5-HT Receptor Metabolic Disease
    Relenopride is a agonist of novel potent 5-HT4 receptor partial with weak binding to 5-HT 2B receptors (Ki = 31 nM) .
    Relenopride
  • HY-162591

    Cholinesterase (ChE) 5-HT Receptor Neurological Disease
    MR33317 is an inhibitor of acetylcholinesterase with an IC50 value of 41nM. MR33317 is also an agonist at brain 5-HT4 receptors .
    MR33317

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