5-HT₄ Receptor Agonist

Cisapride (R 51619) is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

PF-03382792 is a potent 5-HT₄ partial agonist with a K_i of 2.7 nM and an EC₅₀ of 0.9 nM for 5-HT_4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex.

Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pK_is 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.

Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (K_i = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.

Lirexapride is a 5-HT4/Dopamine D2 receptor agonist. Lirexapride stimulants gastrointestinal motor. Lirexapride can be used for research on digestive system disorders.

Cisapride-¹³C,d₃ (R 51619-¹³C,d₃) is the deuterated, ¹³C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

Cisapride-d₆ (R51619-d₆) is the deuterated-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

CSP-2503 is a potent and selective 5-HT_1A receptor agonist , with an EC₅₀ of 0.15 μM and a K_i of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (K_i > 1000 nM), 5-HT₄ receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.

Capeserod hydrochloride (SL65.0155) is a 5-HT_4(e) receptor partial agonist (K_i=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing 5-HT_4(b) and 5-HT_4(e) splice variants, stimulating cAMP production with IC₅₀ values of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia.

TKS 159 is a 5-HT4 receptor agonist. TKS 159 can promote gastrointestinal motility. TKS 159 can be used for research on gastrointestinal conditions.

Minesapride hydrobromide (DSP-6952 hydrobromide) is an orally active, selective 5-HT4 receptor partial agonist. Minesapride hydrobromide enhances gastrointestinal motility, colonic transit and defecation function, and inhibits visceral hypersensitivity. Minesapride hydrobromide does not inhibit/induce cytochrome P450 isozymes, has no significant affinity for hERG, and does not trigger the risk of cardiac ischemia via coronary vasoconstriction. Minesapride hydrobromide can be used in research related to constipation-predominant irritable bowel syndrome, chronic constipation, atonic constipation, spastic constipation, functional constipation and functional dyspepsia.

Minesapride (DSP-6952 free base) is an orally active, selective 5-HT4 receptor partial agonist. Minesapride enhances gastrointestinal motility, colonic transit and defecation function, and inhibits visceral hypersensitivity. Minesapride does not inhibit/induce cytochrome P450 isozymes, has no significant affinity for hERG, and does not trigger the risk of cardiac ischemia via coronary vasoconstriction. Minesapride can be used in research related to constipation-predominant irritable bowel syndrome, chronic constipation, atonic constipation, spastic constipation, functional constipation and functional dyspepsia.

Cisapride (R 51619) (Standard) is the analytical standard of Cisapride (HY-14149). This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

5-HT4R agonist-3 is a 5-HT4R agonist with an EC₅₀ of 22 nM. 5-HT4R agonist-3 selectively modulates 5-HT4R and induces pro-cognitive activity. 5-HT4R agonist-3 can be used in research related to Alzheimer's disease.