Identification
- Name
- Tegaserod
- Accession Number
- DB01079 (APRD00096)
- Type
- Small Molecule
- Groups
- Approved, Investigational, Withdrawn
- Description
Tegaserod is a 5-HT4 agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation. Its use was the only drug approved by the United States Food and Drug Administration to help relieve the abdominal discomfort, bloating and constipation associated with irritable bowel syndrome. On March 30, 2007, the U.S. Food and Drug Administration requested that Novartis withdraw Zelnorm from shelves. The FDA alleges a relationship between prescriptions of the drug and increased risks of heart attack or stroke. [Wikipedia]
- Structure
- Synonyms
- 1-(((5-Methoxyindol-3-yl)methylene)amino)-3-pentylguanidine
- Tegaserod
- tégasérod
- tegaserodum
- External IDs
- SDZ HTF 919
- Product Ingredients
Ingredient UNII CAS InChI Key Tegaserod maleate E5XNT3RF5A 189188-57-6 CPDDZSSEAVLMRY-FEQFWAPWSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Zelnorm Tablet 6 mg/1 Oral Novartis 2002-07-24 2008-06-30 US Zelnorm Tablet 2 mg/1 Oral Novartis 2002-07-24 2010-05-31 US Zelnorm Tablet 6 mg/1 Oral Novartis 2002-07-24 2009-01-31 US - International/Other Brands
- Zelmac / Zelnorm
- Categories
- Alimentary Tract and Metabolism
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Drugs for Constipation
- Gastrointestinal Agents
- Laxatives
- Neurotransmitter Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 4 Receptor Antagonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Agonists
- Serotonin Receptor Antagonists
- Serotonin-4 Receptor Antagonist
- UNII
- 458VC51857
- CAS number
- 145158-71-0
- Weight
- Average: 301.394
Monoisotopic: 301.190260381 - Chemical Formula
- C16H23N5O
- InChI Key
- IKBKZGMPCYNSLU-RGVLZGJSSA-N
- InChI
- InChI=1S/C16H23N5O/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21)/b20-11+
- IUPAC Name
- N'-[(E)-[(5-methoxy-1H-indol-3-yl)methylidene]amino]-N-pentylguanidine
- SMILES
- CCCCCNC(=N)N\N=C\C1=CNC2=C1C=C(OC)C=C2
Pharmacology
- Indication
Provides relief from the symptoms of irritable bowel syndrome including chronic idiopathic constipation.
- Pharmacodynamics
Tegaserod is indicated for the short-term treatment of women with irritable bowel syndrome (IBS) whose primary bowel symptom is constipation. Irritable bowel syndrome with constipation and chronic idiopathic constipation are both lower gastrointestinal dysmotility disorders. Clinical investigations have shown that both motor and sensory functions of the gut appear to be altered in patients suffering from irritable bowel syndrome (IBS), while in patients with chronic idiopathic constipation, reduced intestinal motility is the predominant cause of the condition. Both the enteric nervous system, which acts to integrate and process information in the gut, and 5-hydroxytryptamine (5-HT, serotonin) are thought to represent key elements in the etiology of both IBS and idiopathic constipation. Approximately 95% of serotonin is found throughout the gastrointestinal tract, primarily stored in enterochromaffin cells but also in enteric nerves acting as a neurotransmitter. Serotonin has been shown to be involved in regulating motility, visceral sensitivity and intestinal secretion. Investigations suggest an important role of serotonin Type-4 (5-HT4) receptors in the maintenance of gastrointestinal functions in humans. 5-HT4 receptor mRNA has been found throughout the human gastrointestinal tract.
- Mechanism of action
Tegaserod is a 5-HT4 receptor partial agonist that binds with high affinity at human 5-HT4 receptors, whereas it has no appreciable affinity for 5-HT3 or dopamine receptors. It has moderate affinity for 5-HT1 receptors. Tegaserod, by acting as an agonist at neuronal 5-HT4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. The activation of 5-HT4 receptors in the gastrointestinal tract stimulates the peristaltic reflex and intestinal secretion, as well as inhibits visceral sensitivity.
Target Actions Organism A5-hydroxytryptamine receptor 4 antagonistpartial agonistHumans U5-hydroxytryptamine receptor 2B antagonistHumans U5-hydroxytryptamine receptor 2C antagonistHumans U5-hydroxytryptamine receptor 2A antagonistHumans - Absorption
Rapidly absorbed after oral administration, with an absolute bioavailability of approximately 10%.
- Volume of distribution
- 368 ± 223 L
- Protein binding
98%
- Metabolism
Tegaserod is metabolized mainly via two pathways. The first is a presystemic acid catalyzed hydrolysis in the stomach followed by oxidation and conjugation which produces the main metabolite of tegaserod, 5-methoxyindole-3-carboxylic acid glucuronide. The main metabolite has negligible affinity for 5-HT4 receptors in vitro. The second metabolic pathway of tegaserod is direct glucuronidation which leads to generation of three isomeric N-glucuronides.
- Route of elimination
Approximately two-thirds of the orally administered dose of tegaserod is excreted unchanged in the feces, with the remaining one-third excreted in the urine, primarily as the main metabolite.
- Half life
11 ± 5 hours
- Clearance
- 77 +/- 15 L/h [IV administration]
- Toxicity
Oral LD50 in rat is 2000 mg/kg.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction (R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Tegaserod. (S)-Warfarin The risk or severity of adverse effects can be increased when Tegaserod is combined with (S)-Warfarin. 2,5-Dimethoxy-4-ethylamphetamine The risk or severity of serotonin syndrome can be increased when Tegaserod is combined with 2,5-Dimethoxy-4-ethylamphetamine. 2,5-Dimethoxy-4-ethylthioamphetamine The risk or severity of serotonin syndrome can be increased when Tegaserod is combined with 2,5-Dimethoxy-4-ethylthioamphetamine. 3,4-Methylenedioxyamphetamine The risk or severity of serotonin syndrome can be increased when Tegaserod is combined with 3,4-Methylenedioxyamphetamine. 4-Bromo-2,5-dimethoxyamphetamine The risk or severity of serotonin syndrome can be increased when Tegaserod is combined with 4-Bromo-2,5-dimethoxyamphetamine. 4-hydroxycoumarin The risk or severity of adverse effects can be increased when Tegaserod is combined with 4-hydroxycoumarin. 4-Methoxyamphetamine The metabolism of 4-Methoxyamphetamine can be decreased when combined with Tegaserod. 5-methoxy-N,N-dimethyltryptamine The risk or severity of serotonin syndrome can be increased when Tegaserod is combined with 5-methoxy-N,N-dimethyltryptamine. 6-O-benzylguanine The metabolism of 6-O-benzylguanine can be decreased when combined with Tegaserod. - Food Interactions
- Take before a meal, to increase absorption, take 30 minutes before a meal.
References
- Synthesis Reference
Sundaram Venkataraman, Srinivasulu Gudipati, Brahmeshwararao Mandava Venkata Naga, Goverdhan Banda, Radhakrishna Singamsetty, "Process for preparing form I of tegaserod maleate." U.S. Patent US20050272802, issued December 08, 2005.
US20050272802- General References
- Not Available
- External Links
- KEGG Drug
- D06056
- PubChem Compound
- 5362436
- PubChem Substance
- 46506519
- ChemSpider
- 10609889
- BindingDB
- 79022
- ChEBI
- 51043
- ChEMBL
- CHEMBL76370
- Therapeutic Targets Database
- DAP001526
- PharmGKB
- PA130413154
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Tegaserod
- ATC Codes
- A06AX06 — Tegaserod
- FDA label
- Download (634 KB)
- MSDS
- Download (58.1 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Murfreesboro Pharmaceutical Nursing Supply
- Novartis AG
- Dosage forms
Form Route Strength Tablet Oral 2 mg/1 Tablet Oral 6 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) US5510353 No 1996-04-23 2013-04-26 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 155 °C Not Available logP 2.6 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0288 mg/mL ALOGPS logP 2.76 ALOGPS logP 2.95 ChemAxon logS -4 ALOGPS pKa (Strongest Acidic) 15.24 ChemAxon pKa (Strongest Basic) 8.5 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 4 ChemAxon Polar Surface Area 85.29 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 110.25 m3·mol-1 ChemAxon Polarizability 34.96 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9973 Blood Brain Barrier + 0.7842 Caco-2 permeable - 0.5939 P-glycoprotein substrate Substrate 0.921 P-glycoprotein inhibitor I Non-inhibitor 0.8978 P-glycoprotein inhibitor II Non-inhibitor 0.959 Renal organic cation transporter Inhibitor 0.5488 CYP450 2C9 substrate Non-substrate 0.8522 CYP450 2D6 substrate Non-substrate 0.5492 CYP450 3A4 substrate Non-substrate 0.6565 CYP450 1A2 substrate Non-inhibitor 0.53 CYP450 2C9 inhibitor Non-inhibitor 0.7096 CYP450 2D6 inhibitor Non-inhibitor 0.7807 CYP450 2C19 inhibitor Non-inhibitor 0.6372 CYP450 3A4 inhibitor Non-inhibitor 0.8954 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7654 Ames test Non AMES toxic 0.5434 Carcinogenicity Non-carcinogens 0.7783 Biodegradation Not ready biodegradable 0.9972 Rat acute toxicity 2.6038 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5123 hERG inhibition (predictor II) Non-inhibitor 0.8334
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as indoles. These are compounds containing an indole moiety, which consists of pyrrole ring fused to benzene to form 2,3-benzopyrrole.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Indoles and derivatives
- Sub Class
- Indoles
- Direct Parent
- Indoles
- Alternative Parents
- Anisoles / Alkyl aryl ethers / Substituted pyrroles / Heteroaromatic compounds / Guanidines / Carboximidamides / Azacyclic compounds / Organopnictogen compounds / Imines / Hydrocarbon derivatives
- Substituents
- Indole / Anisole / Alkyl aryl ether / Substituted pyrrole / Benzenoid / Pyrrole / Heteroaromatic compound / Guanidine / Azacycle / Ether
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- guanidines, indoles, carboxamidine, hydrazines (CHEBI:51043)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntagonistPartial agonist
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR4
- Uniprot ID
- Q13639
- Uniprot Name
- 5-hydroxytryptamine receptor 4
- Molecular Weight
- 43760.975 Da
References
- Camilleri M: Review article: tegaserod. Aliment Pharmacol Ther. 2001 Mar;15(3):277-89. [PubMed:11207504]
- Kamm MA: Review article: the complexity of drug development for irritable bowel syndrome. Aliment Pharmacol Ther. 2002 Mar;16(3):343-51. [PubMed:11876686]
- Corsetti M, Tack J: Tegaserod: a new 5-HT(4) agonist in the treatment of irritable bowel syndrome. Expert Opin Pharmacother. 2002 Aug;3(8):1211-8. [PubMed:12150698]
- Beattie DT, Smith JA, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, McCullough JL, Sandlund C, Richardson C, Mai N, Humphrey PP: The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. Epub 2004 Oct 4. [PubMed:15466450]
- Cole P, Rabasseda X: Tegaserod: a serotonin 5-HT4 receptor agonist for treatment of constipation-predominant irritable bowel syndrome. Drugs Today (Barc). 2004 Dec;40(12):1013-30. [PubMed:15645012]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
- Gene Name
- HTR2B
- Uniprot ID
- P41595
- Uniprot Name
- 5-hydroxytryptamine receptor 2B
- Molecular Weight
- 54297.41 Da
References
- Beattie DT, Smith JA, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, McCullough JL, Sandlund C, Richardson C, Mai N, Humphrey PP: The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. Epub 2004 Oct 4. [PubMed:15466450]
- McCullough JL, Armstrong SR, Hegde SS, Beattie DT: The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat. Pharmacol Res. 2006 Apr;53(4):353-8. Epub 2006 Feb 21. [PubMed:16495076]
- Greenwood-Van Meerveld B, Campbell-Dittmeyer K, Johnson AC, Hicks GA: 5-HT2B receptors do not modulate sensitivity to colonic distension in rats with acute colorectal hypersensitivity. Neurogastroenterol Motil. 2006 May;18(5):343-5. [PubMed:16629860]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- Beattie DT, Smith JA, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, McCullough JL, Sandlund C, Richardson C, Mai N, Humphrey PP: The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. Epub 2004 Oct 4. [PubMed:15466450]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Beattie DT, Smith JA, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, McCullough JL, Sandlund C, Richardson C, Mai N, Humphrey PP: The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. Epub 2004 Oct 4. [PubMed:15466450]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Zhou H, Khalilieh S, Svendsen K, Pommier F, Osborne S, Appel-Dingemanse S, Lasseter K, McLeod JF: Tegaserod coadministration does not alter the pharmacokinetics of theophylline in healthy subjects. J Clin Pharmacol. 2001 Sep;41(9):987-93. [PubMed:11549104]
- Vickers AE, Zollinger M, Dannecker R, Tynes R, Heitz F, Fischer V: In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Drug Metab Dispos. 2001 Oct;29(10):1269-76. [PubMed:11560869]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Vickers AE, Zollinger M, Dannecker R, Tynes R, Heitz F, Fischer V: In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Drug Metab Dispos. 2001 Oct;29(10):1269-76. [PubMed:11560869]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Vickers AE, Zollinger M, Dannecker R, Tynes R, Heitz F, Fischer V: In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Drug Metab Dispos. 2001 Oct;29(10):1269-76. [PubMed:11560869]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Serotonin:sodium symporter activity
- Specific Function
- Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- Ismair MG, Kullak-Ublick GA, Blakely RD, Fried M, Vavricka SR: Tegaserod inhibits the serotonin transporter SERT. Digestion. 2007;75(2-3):90-5. Epub 2007 May 18. [PubMed:17510552]
Drug created on June 13, 2005 07:24 / Updated on December 16, 2018 06:46