5-HT4 Selective Agonists | Modulators
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
Tegaserod Maleate is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors.
PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
|Selective||rat 5-HT4E, EC50: 0.62 nM; rat 5-HT4L, EC50: 0.65 nM; rat 5-HT4S, EC50: 0.59 nM; human 5-HT4E, EC50: 0.26 nM; human 5-HT4D, EC50: 0.37 nM; human 5-HT4B, EC50: 0.36 nM; human 5-HT4A, EC50: 0.47 nM|
Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.
|Selective||5-HT4B, Ki: 8 nM; 5-HT4A, Ki: 2.5 nM|
Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
|Selective||5-HT4A, Ki: 2.5 nM; 5-HT4B, Ki: 8 nM|
|S5253||Cisapride (R 51619)||
Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
|Selective||5-HT4 receptor, EC50: 140 nM|
Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
|Selective||5-HT4 receptor, IC50: 0.483 μM|
Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
Mosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
|S5843||Cinitapride Hydrogen Tartrate||
Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors
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