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Results for "

5-HT4

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100170
    5-HT4 antagonist 1

    		5-HT Receptor Neurological Disease
    5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
    <em>5-HT4</em> antagonist 1
  • HY-110094
    BIMU 8

    		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-10457A
    Velusetrag hydrochloride

    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-10457
    Velusetrag

    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-14441
    ML 10302

    		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-103134
    SB 204070A

    		Others 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-103137
    Zacopride hydrochloride

    		5-HT Receptor Neurological Disease
    Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist with Kis of 0.38 and 373 nM for 5-HT3 and 5-HT4 receptor, respectively. Zacopride hydrochloride is also a moderate IK1 channel agonist. Zacopride hydrochloride exerts significant antiarrhythmic and cardiac protective effects .
    Zacopride hydrochloride
  • HY-14149
    Cisapride
    1 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-14442
    ML 10302 hydrochloride

    		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-14149A
    Cisapride monohydrate

    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-101668
    Sulamserod

    RS-100302

    		 5-HT Receptor Cardiovascular Disease
    Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
    Sulamserod
  • HY-101341
    RS 67333 hydrochloride

    		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
    2 Publications Verification

    SB-207266

    		 5-HT Receptor Cardiovascular Disease
    Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.
    Piboserod
  • HY-15574A
    Piboserod hydrochloride

    SB-207266 hydrochloride

    		 5-HT Receptor Cardiovascular Disease
    Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.
    Piboserod hydrochloride
  • HY-14152
    Prucalopride hydrochloride

    		5-HT Receptor Cancer
    Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
    Prucalopride hydrochloride
  • HY-103108
    CJ033466

    		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-101222
    SB-203186 hydrochloride

    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-101638
    (±)-Fabesetron hydrochloride

    (±)-FK1052

    		 5-HT Receptor Neurological Disease
    (±)-Fabesetron hydrochloride ((±)-FK1052) is the racemate of Fabesetron hydrochloride, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist .
    (±)-Fabesetron hydrochloride
  • HY-121826
    Naronapride

    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-102057
    Felcisetrag

    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-U00373
    Revexepride

    		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-U00121
    Lintopride

    		5-HT Receptor Neurological Disease
    Lintopride is a 5HT4 antagonist with moderate 5HT3 antagonist properties.
    Lintopride
  • HY-16729A
    Relenopride hydrochloride

    YKP10811 hydrochloride

    		 5-HT Receptor Inflammation/Immunology
    Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility .
    Relenopride hydrochloride
  • HY-B0189A
    Mosapride citrate
    3 Publications Verification

    TAK-370 citrate; AS-4370 citrate

    		 5-HT Receptor Potassium Channel Cytochrome P450 Neurological Disease Cancer
    Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
    Mosapride citrate
  • HY-B0189S1
    Mosapride-d5

    		Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    Mosapride-d5 is the deuterium labeled Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
    Mosapride-d5
  • HY-148846
    Mosapride N-Oxide

    		Drug Metabolite Metabolic Disease
    Mosapride N-Oxide is a major active metabolite of Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
    Mosapride N-Oxide
  • HY-B2089
    Cinitapride

    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-105201
    Fabesetron

    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-128386
    Cinitapride monotartrate

    		5-HT Receptor Dopamine Receptor Neurological Disease
    Cinitapride monotartrate is a 5-HT1A and 5-HT4 agonist. Cinitapride monotartrate is also a 5-HT2A and D2 antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia .
    Cinitapride monotartrate
  • HY-101172
    RS 23597-190

    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 5-HT-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .
    RS 23597-190
  • HY-116565
    Usmarapride

    SUVN-D4010

    		 5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
    Usmarapride
  • HY-14147
    Renzapride

    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-116565A
    Usmarapride free base

    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-44132
    Dehydro Palonosetron

    RS 42358-197

    		 5-HT Receptor Neurological Disease
    Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors .
    Dehydro Palonosetron
  • HY-14153AS
    Tegaserod-13C,d3 maleate

    SDZ-HTF-919-13C,d3; HTF-919-13C,d3

    		 Isotope-Labeled Compounds 5-HT Receptor Neurological Disease Metabolic Disease
    Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
    Tegaserod-13C,d3 maleate
  • HY-18137
    PF-04995274

    		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-14147A
    (S)-Renzapride

    (S)-BRL 24924

    		 5-HT Receptor Metabolic Disease
    (S)-Renzapride ((S)-BRL 24924) is the isomer of HY-14147 Renzapride. Renzapride is a 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride also is a 5HT2b and 5HT3 receptor antagonist. Renzapride can be used for constipation predominant irritable bowel syndrome (C-IBS) study .
    (S)-Renzapride
  • HY-101653
    MHP 133

    		Cholinesterase (ChE) mAChR 5-HT Receptor Neurological Disease
    MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
    MHP 133
  • HY-12694
    Prucalopride succinate
    2 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-101343
    RS 39604

    		5-HT Receptor Neurological Disease
    RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
    RS 39604
  • 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-10564S
    Sarpogrelate-d3 hydrochloride

    MCI-9042-d3

    		 Isotope-Labeled Compounds 5-HT Receptor Cardiovascular Disease
    Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. 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[1][2][3].
    Sarpogrelate-d3 hydrochloride
  • HY-B0189
    Mosapride

    TAK-370; AS-4370

    		 5-HT Receptor Cytochrome P450 Potassium Channel Neurological Disease Cancer
    Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
    Mosapride
  • HY-103146
    GR125487 sulfamate

    		5-HT Receptor Neurological Disease
    GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction .
    GR125487 sulfamate
  • HY-14151
    Prucalopride
    2 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

    		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-14153
    Tegaserod

    		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

    SDZ-HTF-919; HTF-919

    		 5-HT Receptor Apoptosis Neurological Disease Metabolic Disease
    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-134807
    Indophagolin

    		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

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