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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
43 Results for "
5-HT4 receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (43)
43 Results for "5-HT4 receptor antagonist" in MCE Product Catalog:
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9 Publications Verification
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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 .
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4 Cited Publications
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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 .
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4 Cited Publications
Synonyms: SDZ-HTF-919; HTF-919
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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 .
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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) .
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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 .
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1 Cited Publications
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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 .
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1 Cited Publications
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5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
Synonyms: EP-A-501322
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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 .
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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 .
Cat. No.: HY-B2089
CAS No.: 66564-14-5
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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 .
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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 .
Cat. No.: HY-135439
CAS No.: 135938-17-9
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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 .
Cat. No.: HY-101668
CAS No.: 219757-90-1
Synonyms: RS-100302
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Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
Synonyms: BRL 24924
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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 .
Cat. No.: HY-15574A
CAS No.: 178273-87-5
Synonyms: SB-207266 hydrochloride
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Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.
Cat. No.: HY-105201
CAS No.: 129300-27-2
Synonyms: FK1052 free base
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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 .
Cat. No.: HY-B2089R
CAS No.: 66564-14-5
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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 .
Cat. No.: HY-W822786
CAS No.: 144625-67-2
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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 .
Cat. No.: HY-10564R
CAS No.: 135159-51-2
Synonyms: MCI-9042 (Standard)
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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 .
Cat. No.: HY-103134
CAS No.: 148688-01-1
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
