Home Neuronal Signaling 5-HT Receptor agonist Tegaserod Maleate For research use only.

Tegaserod Maleate

Synonyms: HTF-919

Tegaserod Maleate(HTF-919) 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.

Tegaserod Maleate Chemical Structure

Tegaserod Maleate Chemical Structure

CAS No. 189188-57-6

Purity & Quality Control

Batch: S540101 DMSO]83 mg/mL]false]Ethanol]8 mg/mL]false]Water]Insoluble]false Purity: 99.89%
99.89

Tegaserod Maleate Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Tegaserod Maleate(HTF-919) 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.
Targets
5-HT4 receptor [1]
In vitro
In vitro

In guinea-pig and rat colon, luminal application of tegaserod activates 5-HT4 receptors on intrinsic primary sensory neurons that release calcitonin gene-related peptide which in turn activates cholinergic interneurons stimulating the peristaltic reflex. In isolated segments of guinea-pig colon, intralumnal tegaserod increased the velocity of propulsion of artificial faecal pellets through the stimulation of the same receptor. In rat distal colon, intraluminal tegaserod stimulated 5-HT4 4 receptors on colonocytes to secrete chloride and water through an adenylyl cyclase-dependent pathway[1].
In Vivo
In vivo

In a study in dogs tegaserod 0.1 or 0.3 mg/kg i.v. increased the motility of the antrum, duodenum and jejunum in both fasting and fed conditions. In a model of delayed gastric emptying, the same doses of tegaserod restored normal gastric transit time. Tegaserod 0.3 mg/kg in rats was able to increase gastric and small bowel motility while in a model of postoperative ileus it was able to restore gastric motility. In humans, pharmacokinetic analysis reveals that tegaserod is rapidly absorbed following oral administration. Absolute bioavailability is 11 ± 3% and is decreased by 50% under fed conditions. The time to reach peak plasma concentration ranges from 1-1.3 h. In the bloodstream, tegaserod is predominantly bound by α1-glycoprotein and does not cross the blood-brain barrier to any significant extent. The terminal elimination half time is 11 ± 5 h. Age and gender do not influence the pharmacokinetics of tegaserod and tegaserod has the potential for good tolerability[1].

Chemical Information & Solubility

Molecular Weight 417.46 Formula

C16H23N5O.C4H4O4
CAS No. 189188-57-6 SDF --
Smiles CCCCCN=C(N)NN=CC1=CNC2=C1C=C(C=C2)OC.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 83 mg/mL ( (198.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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