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Identification
NameTegaserod
Accession NumberDB01079  (APRD00096)
TypeSmall Molecule
GroupsInvestigational, Withdrawn
DescriptionTegaserod 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
Thumb
Synonyms
1-(((5-Methoxyindol-3-yl)methylene)amino)-3-pentylguanidine
tégasérod
tegaserodum
External Identifiers
  • SDZ HTF 919
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ZelmacNot Available
ZelnormNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tegaserod maleate
189188-57-6
Thumb
  • InChI Key: CPDDZSSEAVLMRY-FEQFWAPWSA-N
  • Monoisotopic Mass: 417.201218989
  • Average Mass: 417.466
DBSALT001797
Categories
UNII458VC51857
CAS number145158-71-0
WeightAverage: 301.394
Monoisotopic: 301.190260381
Chemical FormulaC16H23N5O
InChI KeyIKBKZGMPCYNSLU-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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndoles
Direct ParentIndoles
Alternative Parents
Substituents
  • Indole
  • Anisole
  • Phenol ether
  • Alkyl aryl ether
  • Substituted pyrrole
  • Benzenoid
  • Pyrrole
  • Heteroaromatic compound
  • Guanidine
  • Carboximidamide
  • Ether
  • Azacycle
  • Organic nitrogen compound
  • Organooxygen compound
  • Organonitrogen compound
  • Hydrocarbon derivative
  • Imine
  • Organic oxygen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationProvides relief from the symptoms of irritable bowel syndrome including chronic idiopathic constipation.
PharmacodynamicsTegaserod 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 actionTegaserod 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.
Related Articles
AbsorptionRapidly absorbed after oral administration, with an absolute bioavailability of approximately 10%.
Volume of distribution
  • 368 ± 223 L
Protein binding98%
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 eliminationApproximately 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 life11 ± 5 hours
Clearance
  • 77 +/- 15 L/h [IV administration]
ToxicityOral LD50 in rat is 2000 mg/kg.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9973
Blood Brain Barrier+0.7842
Caco-2 permeable-0.5939
P-glycoprotein substrateSubstrate0.921
P-glycoprotein inhibitor INon-inhibitor0.8978
P-glycoprotein inhibitor IINon-inhibitor0.959
Renal organic cation transporterInhibitor0.5488
CYP450 2C9 substrateNon-substrate0.8522
CYP450 2D6 substrateNon-substrate0.5492
CYP450 3A4 substrateNon-substrate0.6565
CYP450 1A2 substrateNon-inhibitor0.53
CYP450 2C9 inhibitorNon-inhibitor0.7096
CYP450 2D6 inhibitorNon-inhibitor0.7807
CYP450 2C19 inhibitorNon-inhibitor0.6372
CYP450 3A4 inhibitorNon-inhibitor0.8954
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7654
Ames testNon AMES toxic0.5434
CarcinogenicityNon-carcinogens0.7783
BiodegradationNot ready biodegradable0.9972
Rat acute toxicity2.6038 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5123
hERG inhibition (predictor II)Non-inhibitor0.8334
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage formsNot Available
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5510353 No1993-04-262013-04-26Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point155 °CNot Available
logP2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0288 mg/mLALOGPS
logP2.76ALOGPS
logP2.95ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)15.24ChemAxon
pKa (Strongest Basic)8.5ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area85.29 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity110.25 m3·mol-1ChemAxon
Polarizability34.96 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
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 ReferencesNot Available
External Links
ATC CodesA06AX06
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (634 KB)
MSDSDownload (58.1 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe metabolism of Tegaserod can be decreased when combined with Abiraterone.
AmiodaroneThe metabolism of Tegaserod can be decreased when combined with Amiodarone.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Tegaserod.
ArtemetherThe metabolism of Tegaserod can be decreased when combined with Artemether.
AtomoxetineThe metabolism of Tegaserod can be decreased when combined with Atomoxetine.
BetaxololThe metabolism of Tegaserod can be decreased when combined with Betaxolol.
BupropionThe metabolism of Tegaserod can be decreased when combined with Bupropion.
CelecoxibThe metabolism of Tegaserod can be decreased when combined with Celecoxib.
ChloroquineThe metabolism of Tegaserod can be decreased when combined with Chloroquine.
ChlorpromazineThe metabolism of Tegaserod can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Tegaserod can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Tegaserod can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Tegaserod can be decreased when combined with Cinacalcet.
CitalopramThe metabolism of Tegaserod can be decreased when combined with Citalopram.
ClemastineThe metabolism of Tegaserod can be decreased when combined with Clemastine.
ClobazamThe metabolism of Tegaserod can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Tegaserod can be decreased when combined with Clomipramine.
ClotrimazoleThe metabolism of Tegaserod can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Tegaserod can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Tegaserod can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Tegaserod can be decreased when combined with Cocaine.
DarifenacinThe metabolism of Tegaserod can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Tegaserod can be increased when it is combined with Darunavir.
DelavirdineThe metabolism of Tegaserod can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Tegaserod can be decreased when combined with Desipramine.
DiphenhydramineThe metabolism of Tegaserod can be decreased when combined with Diphenhydramine.
DronedaroneThe metabolism of Tegaserod can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Tegaserod can be decreased when combined with Duloxetine.
EliglustatThe metabolism of Tegaserod can be decreased when combined with Eliglustat.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tegaserod.
FluoxetineThe metabolism of Tegaserod can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Tegaserod can be decreased when combined with Fluvoxamine.
HaloperidolThe metabolism of Tegaserod can be decreased when combined with Haloperidol.
ImipramineThe metabolism of Tegaserod can be decreased when combined with Imipramine.
IndinavirThe metabolism of Tegaserod can be decreased when combined with Indinavir.
IsoniazidThe metabolism of Tegaserod can be decreased when combined with Isoniazid.
KetoconazoleThe metabolism of Tegaserod can be decreased when combined with Ketoconazole.
LopinavirThe metabolism of Tegaserod can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Tegaserod can be decreased when combined with Lorcaserin.
LumefantrineThe metabolism of Tegaserod can be decreased when combined with Lumefantrine.
MethadoneThe metabolism of Tegaserod can be decreased when combined with Methadone.
MethotrimeprazineThe metabolism of Tegaserod can be decreased when combined with Methotrimeprazine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Tegaserod.
MetoprololThe metabolism of Tegaserod can be decreased when combined with Metoprolol.
MirabegronThe metabolism of Tegaserod can be decreased when combined with Mirabegron.
NevirapineThe metabolism of Tegaserod can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Tegaserod can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Tegaserod can be decreased when combined with Nilotinib.
PanobinostatThe metabolism of Tegaserod can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Tegaserod can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Tegaserod can be decreased when it is combined with Peginterferon alfa-2b.
PromazineThe metabolism of Tegaserod can be decreased when combined with Promazine.
QuinidineThe metabolism of Tegaserod can be decreased when combined with Quinidine.
QuinineThe metabolism of Tegaserod can be decreased when combined with Quinine.
RanolazineThe metabolism of Tegaserod can be decreased when combined with Ranolazine.
RitonavirThe metabolism of Tegaserod can be decreased when combined with Ritonavir.
RolapitantThe metabolism of Tegaserod can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Tegaserod can be decreased when combined with Ropinirole.
SertralineThe metabolism of Tegaserod can be decreased when combined with Sertraline.
StiripentolThe metabolism of Tegaserod can be decreased when combined with Stiripentol.
TerbinafineThe metabolism of Tegaserod can be decreased when combined with Terbinafine.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Tegaserod.
ThioridazineThe metabolism of Tegaserod can be decreased when combined with Thioridazine.
TiclopidineThe metabolism of Tegaserod can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Tegaserod can be decreased when combined with Tipranavir.
TranylcypromineThe metabolism of Tegaserod can be decreased when combined with Tranylcypromine.
VenlafaxineThe metabolism of Tegaserod can be decreased when combined with Venlafaxine.
ZiprasidoneThe metabolism of Tegaserod can be decreased when combined with Ziprasidone.
Food Interactions
  • Take before a meal, to increase absorption, take 30 minutes before a meal.

Targets

Kind
Protein
Organism
Human
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 is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR4
Uniprot ID:
Q13639
Molecular Weight:
43760.975 Da
References
  1. Camilleri M: Review article: tegaserod. Aliment Pharmacol Ther. 2001 Mar;15(3):277-89. [PubMed:11207504 ]
  2. Kamm MA: Review article: the complexity of drug development for irritable bowel syndrome. Aliment Pharmacol Ther. 2002 Mar;16(3):343-51. [PubMed:11876686 ]
  3. 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 ]
  4. 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 ]
  5. 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 ]
  6. 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
Human
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 change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
References
  1. 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 ]
  2. 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 ]
  3. 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
Human
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-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. 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
Human
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-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. 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
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. 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 ]

Transporters

Kind
Protein
Organism
Human
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 the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23