Identification

Name
Vardenafil
Accession Number
DB00862  (APRD00699)
Type
Small Molecule
Groups
Approved
Description

Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Structure
Thumb
Synonyms
  • 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-F][1,2,4]triazin-4(1H)-one
  • Vardénafil
  • Vardenafil
  • Vardenafilo
  • Vardenafilum
External IDs
BAY 389456 / BAY-389456 / BAY38-9456 / DE 19750085 1997 / WO 99/24433 1999
Product Ingredients
IngredientUNIICASInChI Key
Vardenafil hydrochloride5M8S2CU0TS330808-88-3FBCDRHDULQYRTB-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LevitraTablet, film coated10 mg/1OralSchering Plough2008-05-152013-07-01Us
LevitraTablet, orally disintegrating10 mgOralBayer Ag2003-03-06Not applicableEu
LevitraTablet5 mgOralBayer2004-03-17Not applicableCanada
LevitraTablet, film coated20 mgOralBayer Ag2003-03-06Not applicableEu
LevitraTablet, film coated20 mgOralBayer Ag2003-03-06Not applicableEu
LevitraTablet, film coated20 mg/1OralPD-Rx Pharmaceuticals, Inc.2003-08-25Not applicableUs
LevitraTablet, film coated5 mgOralBayer Ag2003-03-06Not applicableEu
LevitraTablet, film coated20 mg/1OralAphena Pharma Solutions Tennessee, Inc.2008-05-15Not applicableUs
LevitraTablet, film coated10 mg/1OralGlaxoSmithKline LLC2003-08-25Not applicableUs0173 083020180907 15195 koi6rk
LevitraTablet, film coated10 mgOralBayer Ag2003-03-06Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
VardenafilTablet, film coated5 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-11-01Not applicableUs
VardenafilTablet, film coated20 mg/1OralCadila Healthcare Limited2018-11-01Not applicableUs
VardenafilTablet, film coated2.5 mg/1OralCadila Healthcare Limited2018-11-01Not applicableUs
VardenafilTablet, film coated20 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-11-01Not applicableUs
VardenafilTablet, film coated2.5 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-11-01Not applicableUs
VardenafilTablet, film coated10 mg/1OralCadila Healthcare Limited2018-11-01Not applicableUs
VardenafilTablet, film coated10 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-11-01Not applicableUs
VardenafilTablet, film coated5 mg/1OralCadila Healthcare Limited2018-11-01Not applicableUs
Vardenafil HydrochlorideTablet, film coated20 mg/1OralTeva Pharmaceuticals USA, Inc.2018-10-03Not applicableUs
Vardenafil hydrochlorideTablet, film coated10 mg/1OralAmneal Pharmaceuticals LLC2018-10-31Not applicableUs
International/Other Brands
Levitra / Vivanza (GlaxoSmithKline)
Categories
UNII
UCE6F4125H
CAS number
224785-90-4
Weight
Average: 488.603
Monoisotopic: 488.220574232
Chemical Formula
C23H32N6O4S
InChI Key
SECKRCOLJRRGGV-UHFFFAOYSA-N
InChI
InChI=1S/C23H32N6O4S/c1-5-8-20-24-16(4)21-23(30)25-22(26-29(20)21)18-15-17(9-10-19(18)33-7-3)34(31,32)28-13-11-27(6-2)12-14-28/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,30)
IUPAC Name
2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propyl-1H,4H-imidazo[4,3-f][1,2,4]triazin-4-one
SMILES
CCCC1=NC(C)=C2N1NC(=NC2=O)C1=C(OCC)C=CC(=C1)S(=O)(=O)N1CCN(CC)CC1

Pharmacology

Indication

Used for the treatment of erectile dysfunction

Associated Conditions
Pharmacodynamics

Vardenafil is used to treat male erectile dysfunction (impotence) and pulmonary arterial hypertension (PAH). Part of the physiological process of erection involves the release of nitric oxide (NO) in the corpus cavernosum. This then activates the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP), leading to smooth muscle relaxation in the corpus cavernosum, resulting in increased inflow of blood and an erection. Vardenafil is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. This means that, with vardenafil on board, normal sexual stimulation leads to increased levels of cGMP in the corpus cavernosum which leads to better erections. Without sexual stimulation and no activation of the NO/cGMP system, vardenafil should not cause an erection.

Mechanism of action

Vardenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by vardenafil enhances erectile function by increasing the amount of cGMP.

TargetActionsOrganism
AcGMP-specific 3',5'-cyclic phosphodiesterase
inhibitor
Human
URetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
allosteric modulator
Human
URetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
allosteric modulator
Human
Absorption

Vardenafil is rapidly absorbed with absolute bioavailability of approximately 15%.

Volume of distribution
  • 208 L
Protein binding

95%

Metabolism

Vardenafil is metabolized predominantly by the hepatic enzyme CYP3A4, with contribution from the CYP3A5 and CYP2C isoforms. The major circulating metabolite, M1, results from desethylation at the piperazine moiety of vardenafil. M1 shows a phosphodiesterase selectivity profile similar to that of vardenafil and an in vitro inhibitory potency for PDE5 28% of that of vardenafil.

Route of elimination

After oral administration, vardenafil is excreted as metabolites predominantly in the feces (approximately 91-95% of administered oral dose) and to a lesser extent in the urine (approximately 2-6% of administered oral dose).

Half life

4-5 hours

Clearance
  • 56 L/h
Toxicity

Symptoms of overdose include vision changes and back and muscle pain.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of Vardenafil can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of Vardenafil can be decreased when combined with (S)-Warfarin.
3,5-diiodothyropropionic acidThe metabolism of Vardenafil can be decreased when combined with 3,5-diiodothyropropionic acid.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Vardenafil.
5-androstenedioneThe metabolism of Vardenafil can be decreased when combined with 5-androstenedione.
6-Deoxyerythronolide BThe metabolism of Vardenafil can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of Vardenafil can be decreased when combined with 6-O-benzylguanine.
AbemaciclibThe metabolism of Vardenafil can be decreased when combined with Abemaciclib.
AbexinostatThe risk or severity of QTc prolongation can be increased when Vardenafil is combined with Abexinostat.
AbirateroneThe metabolism of Vardenafil can be decreased when combined with Abiraterone.
Food Interactions
Not Available

References

Synthesis Reference

Yogesh S. Deshpande, Sandra Brueck, Julia Schulze Nahrup, Birgit Schnitter, Ganesh Gat, Javed Hussain, "PROCESS FOR THE PREPARATION OF A MEDICAMENT COMPRISING VARDENAFIL HYDROCHLORIDE TRIHYDRATE." U.S. Patent US20100159003, issued June 24, 2010.

US20100159003
General References
Not Available
External Links
Human Metabolome Database
HMDB0015000
KEGG Drug
D09989
PubChem Compound
110634
PubChem Substance
46506777
ChemSpider
99300
BindingDB
50088373
ChEBI
46295
ChEMBL
CHEMBL1520
Therapeutic Targets Database
DAP000414
PharmGKB
PA10229
HET
VDN
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Vardenafil
ATC Codes
G04BE09 — Vardenafil
AHFS Codes
  • 24:12.12 — Phosphodiesterase Type 5 Inhibitors
PDB Entries
1uho / 1xot / 1xp0 / 3b2r
FDA label
Download (535 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0TerminatedTreatmentBrain Metastasis / Gliomas / Neoplasms, Brain1
1CompletedNot AvailableErectile Dysfunction (ED)2
1CompletedBasic ScienceGenetic Polymorphic CYP3A5 / Healthy Volunteers / Pharmacokinetics of Three PDE5Is1
1CompletedTreatmentIschemia-Reperfusion Injury1
2CompletedSupportive CareEndothelial Dysfunction / Erectile Dysfunction (ED) / Type 2 Diabetes Mellitus1
2CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
2CompletedTreatmentDetrusor Overactivity / Urinary Bladder, Overactive1
2CompletedTreatmentErectile Dysfunction (ED)2
2CompletedTreatmentProstatic Hypertrophy, Benign1
2CompletedTreatmentTinnitus1
2SuspendedTreatmentCystic Fibrosis (CF)1
2, 3CompletedTreatmentErectile Dysfunction (ED)1
2, 3CompletedTreatmentRaynaud's Syndrome1
3CompletedTreatmentDepression / Erectile Dysfunction (ED)1
3CompletedTreatmentDiabetes Mellitus (DM) / Erectile Dysfunction (ED)1
3CompletedTreatmentErectile Dysfunction (ED)17
3CompletedTreatmentErectile Dysfunction (ED) / Sexual Dysfunction, Physiological1
3CompletedTreatmentErectile Dysfunction (ED) / Sexual Dysfunctions / Spinal Cord Injuries (SCI)1
3CompletedTreatmentPulmonary Hypertension (PH)1
4CompletedNot AvailableErectile Dysfunction (ED)1
4CompletedTreatmentAcquired Immune Deficiency Syndrome (AIDS)1
4CompletedTreatmentArterial Hypertension / Endothelial Dysfunction / Erectile Dysfunction (ED)1
4CompletedTreatmentErectile Dysfunction (ED)15
4CompletedTreatmentErectile Dysfunction (ED) / Metabolic Syndromes1
4CompletedTreatmentErectile Dysfunction (ED) / Spinal Cord Injuries (SCI)1
4CompletedTreatmentMale Erectile Dysfunction / Sexual Dysfunctions1
4CompletedTreatmentSafety1
4RecruitingTreatmentErectile Dysfunction (ED) / Liver Cirrhosis1
4Unknown StatusTreatmentErectile Dysfunction (ED)2
4Unknown StatusTreatmentErectile Dysfunction (ED) / Hypogonadotrophic Males1
4Unknown StatusTreatmentHypogonadism / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentPulmonary Arterial Hypertension (PAH)2
Not AvailableCompletedNot AvailableErectile Dysfunction (ED)4
Not AvailableCompletedTreatmentErectile Dysfunction (ED) / Prostatic Hyperplasia1
Not AvailableTemporarily Not AvailableNot AvailableCoronary Artery Disease / Therapy Refractory Myocardial Ischemia / Unsuitable for Surgical or Percutaneous Revascularisation1
Not AvailableTerminatedNot AvailableErectile Dysfunction (ED)1

Pharmacoeconomics

Manufacturers
  • Bayer healthcare pharmaceuticals inc
Packagers
  • A-S Medication Solutions LLC
  • Bayer Healthcare
  • Bryant Ranch Prepack
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Physicians Total Care Inc.
  • Prepak Systems Inc.
  • Redpharm Drug
  • Schering Corp.
  • Va Cmop Dallas
Dosage forms
FormRouteStrength
TabletOral10 mg
TabletOral20 mg
TabletOral5 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral10 mg
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral20 mg/1
Tablet, film coatedOral20 mg
Tablet, film coatedOral5 mg/1
Tablet, film coatedOral5 mg
Tablet, orally disintegratingOral10 mg
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral11.85 mg/1
TabletOral10 mg/1
TabletOral2.5 mg/1
TabletOral20 mg/1
TabletOral5 mg/1
Prices
Unit descriptionCostUnit
Levitra 10 mg tablet19.04USD tablet
Levitra 20 mg tablet19.04USD tablet
Levitra 5 mg tablet19.04USD tablet
Levitra 2.5 mg tablet18.66USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2309332No2002-12-032018-10-31Canada
US6362178No2002-03-262018-10-31Us
US7696206No2010-04-132018-10-31Us
US8273876No2012-09-252027-07-23Us
US8841446No2014-09-232023-07-03Us
US8613950No2013-12-242028-12-23Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)192 °CNot Available
water solubility0.11 mg/mL (HCl salt)Not Available
logP1.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.325 mg/mLALOGPS
logP2.18ALOGPS
logP1.33ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)8.01ChemAxon
pKa (Strongest Basic)6.21ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area109.13 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity142.71 m3·mol-1ChemAxon
Polarizability53.22 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.6682
Caco-2 permeable+0.5502
P-glycoprotein substrateSubstrate0.7415
P-glycoprotein inhibitor IInhibitor0.6976
P-glycoprotein inhibitor IIInhibitor0.8552
Renal organic cation transporterNon-inhibitor0.6975
CYP450 2C9 substrateNon-substrate0.6386
CYP450 2D6 substrateSubstrate0.7909
CYP450 3A4 substrateSubstrate0.697
CYP450 1A2 substrateNon-inhibitor0.8215
CYP450 2C9 inhibitorInhibitor0.7426
CYP450 2D6 inhibitorNon-inhibitor0.8464
CYP450 2C19 inhibitorNon-inhibitor0.7472
CYP450 3A4 inhibitorInhibitor0.8857
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7205
Ames testNon AMES toxic0.5748
CarcinogenicityNon-carcinogens0.6141
BiodegradationNot ready biodegradable0.8875
Rat acute toxicity2.6208 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8367
hERG inhibition (predictor II)Inhibitor0.7696
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-000i-0040900000-a78a646244f2fb1f6276
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000f-0011900000-88f62b9a8f7aec917a41
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-0092000000-cf98ecae287c01370dbc

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzenesulfonamides. These are organic compounds containing a sulfonamide group that is S-linked to a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzenesulfonamides
Direct Parent
Benzenesulfonamides
Alternative Parents
Benzenesulfonyl compounds / Phenoxy compounds / Phenol ethers / N-alkylpiperazines / Alkyl aryl ethers / Organosulfonamides / N-substituted imidazoles / 1,2,4-triazines / Sulfonyls / Heteroaromatic compounds
show 5 more
Substituents
Benzenesulfonamide / Benzenesulfonyl group / Phenoxy compound / Phenol ether / Alkyl aryl ether / N-alkylpiperazine / 1,4-diazinane / N-substituted imidazole / Piperazine / Organosulfonic acid amide
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-alkylpiperazine, imidazotriazine, N-sulfonylpiperazine (CHEBI:46295)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, ...
Gene Name
PDE5A
Uniprot ID
O76074
Uniprot Name
cGMP-specific 3',5'-cyclic phosphodiesterase
Molecular Weight
99984.14 Da
References
  1. Blount MA, Zoraghi R, Ke H, Bessay EP, Corbin JD, Francis SH: A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization. Mol Pharmacol. 2006 Nov;70(5):1822-31. Epub 2006 Aug 22. [PubMed:16926278]
  2. Carrier S: Pharmacology of phosphodiesterase 5 inhibitors. Can J Urol. 2003 Feb;10 Suppl 1:12-6. [PubMed:12625845]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  4. Kim NN, Huang YH, Goldstein I, Bischoff E, Traish AM: Inhibition of cyclic GMP hydrolysis in human corpus cavernosum smooth muscle cells by vardenafil, a novel, selective phosphodiesterase type 5 inhibitor. Life Sci. 2001 Sep 28;69(19):2249-56. [PubMed:11669467]
  5. Saenz de Tejada I, Angulo J, Cuevas P, Fernandez A, Moncada I, Allona A, Lledo E, Korschen HG, Niewohner U, Haning H, Pages E, Bischoff E: The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90. [PubMed:11890515]
  6. Scheen AJ: [Medication of the month. Vardenafil (Levitra)]. Rev Med Liege. 2003 Sep;58(9):576-9. [PubMed:14626653]
  7. Sung BJ, Hwang KY, Jeon YH, Lee JI, Heo YS, Kim JH, Moon J, Yoon JM, Hyun YL, Kim E, Eum SJ, Park SY, Lee JO, Lee TG, Ro S, Cho JM: Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules. Nature. 2003 Sep 4;425(6953):98-102. [PubMed:12955149]
  8. Wang H, Ye M, Robinson H, Francis SH, Ke H: Conformational variations of both phosphodiesterase-5 and inhibitors provide the structural basis for the physiological effects of vardenafil and sildenafil. Mol Pharmacol. 2008 Jan;73(1):104-10. Epub 2007 Oct 24. [PubMed:17959709]
  9. Zoraghi R, Francis SH, Corbin JD: Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitors. Biochemistry. 2007 Nov 27;46(47):13554-63. Epub 2007 Nov 3. [PubMed:17979301]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Allosteric modulator
General Function
Enzyme inhibitor activity
Specific Function
Participates in processes of transmission and amplification of the visual signal. cGMP-PDEs are the effector molecules in G-protein-mediated phototransduction in vertebrate rods and cones.
Gene Name
PDE6G
Uniprot ID
P18545
Uniprot Name
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Molecular Weight
9643.09 Da
References
  1. Zhang XJ, Cahill KB, Elfenbein A, Arshavsky VY, Cote RH: Direct allosteric regulation between the GAF domain and catalytic domain of photoreceptor phosphodiesterase PDE6. J Biol Chem. 2008 Oct 31;283(44):29699-705. doi: 10.1074/jbc.M803948200. Epub 2008 Sep 8. [PubMed:18779324]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Allosteric modulator
General Function
Enzyme inhibitor activity
Specific Function
Participates in processes of transmission and amplification of the visual signal. cGMP-PDEs are the effector molecules in G-protein-mediated phototransduction in vertebrate rods and cones.
Gene Name
PDE6H
Uniprot ID
Q13956
Uniprot Name
Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Molecular Weight
9074.36 Da
References
  1. Zhang XJ, Cahill KB, Elfenbein A, Arshavsky VY, Cote RH: Direct allosteric regulation between the GAF domain and catalytic domain of photoreceptor phosphodiesterase PDE6. J Biol Chem. 2008 Oct 31;283(44):29699-705. doi: 10.1074/jbc.M803948200. Epub 2008 Sep 8. [PubMed:18779324]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-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 performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 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
Substrate
General Function
Oxygen binding
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
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 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]

Drug created on June 13, 2005 07:24 / Updated on November 20, 2018 00:48