Identification

Name
Bimatoprost
Accession Number
DB00905  (APRD00826, DB06863)
Type
Small Molecule
Groups
Approved, Investigational
Description

Bimatoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes. It binds to the prostanoid FP receptor.

Structure
Thumb
Synonyms
  • (Z)-7-((1R,2R,3R,5S)-3,5-Dihydroxy-2-((1e,3S)-3-hydroxy-5-phenyl-1-pentenyl)cyclopentyl)-N-ethyl-5-heptenamide
  • bimatoprost
  • Bimatoprostum
External IDs
AGN 192024 / AGN-192024
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LatisseSolution / drops0.3 mg/1mLOphthalmicAllergan2009-01-26Not applicableUs
LatisseSolution / drops0.3 mg/1mLOphthalmicPhysicians Total Care, Inc.2009-07-242013-06-30Us
LatisseSolution0.03 %TopicalAllergan2010-11-01Not applicableCanada
LumiganSolution / drops0.1 mg/1mLOphthalmicPhysicians Total Care, Inc.2011-09-14Not applicableUs
LumiganSolution0.3 mg/1mLOphthalmicAllergan, Inc.2006-11-132006-11-13Us
LumiganSolution0.03 %OphthalmicAllergan2002-05-24Not applicableCanada
LumiganSolution / drops0.1 mg/1mLOphthalmicAllergan2010-09-10Not applicableUs
LumiganSolution / drops0.3 mg/1mLOphthalmicPhysicians Total Care, Inc.2001-03-22Not applicableUs
Lumigan PFSolution0.03 %OphthalmicAllerganNot applicableNot applicableCanada
Lumigan RcSolution0.01 %OphthalmicAllergan2009-06-16Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-bimatoprostSolution0.03 %OphthalmicApotex CorporationNot applicableNot applicableCanada
Apo-bimatoprostSolution0.03 %TopicalApotex CorporationNot applicableNot applicableCanada
BimatoprostSolution / drops0.3 mg/1mLOphthalmicLupin Pharmaceuticals2015-05-13Not applicableUs
BimatoprostSolution3 ug/1mLTopicalHi-Tech Pharmacal Co., Inc.2018-10-10Not applicableUs
BimatoprostSolution / drops0.3 mg/1mLOphthalmicSandoz2016-12-06Not applicableUs
BimatoprostSolution / drops0.3 mg/1mLOphthalmicHi-Tech Pharmacal Co., Inc.2018-11-12Not applicableUs
BimatoprostSolution / drops0.3 mg/1mLOphthalmicLupin Pharmaceuticals2015-05-13Not applicableUs
BimatoprostSolution / drops0.3 mg/1mLOphthalmicApotex Corp.2018-10-08Not applicableUs
Categories
UNII
QXS94885MZ
CAS number
155206-00-1
Weight
Average: 415.5656
Monoisotopic: 415.272258677
Chemical Formula
C25H37NO4
InChI Key
AQOKCDNYWBIDND-FTOWTWDKSA-N
InChI
InChI=1S/C25H37NO4/c1-2-26-25(30)13-9-4-3-8-12-21-22(24(29)18-23(21)28)17-16-20(27)15-14-19-10-6-5-7-11-19/h3,5-8,10-11,16-17,20-24,27-29H,2,4,9,12-15,18H2,1H3,(H,26,30)/b8-3-,17-16+/t20-,21+,22+,23-,24+/m0/s1
IUPAC Name
(5Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-phenylpent-1-en-1-yl]cyclopentyl]-N-ethylhept-5-enamide
SMILES
CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1

Pharmacology

Indication

For the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension who are intolerant of other intraocular pressure lowering medications or insufficiently responsive (failed to achieve target IOP determined after multiple measurements over time) to another intraocular pressure lowering medication.

Associated Conditions
Pharmacodynamics

Bimatoprost is a prostamide, a synthetic structural analog of prostaglandin with ocular hypotensive activity, that is chemically related to prostamide F. It selectively mimics the effects of naturally occurring substances, prostamides. Bimatoprost lowers intraocular pressure (IOP) in humans. Elevated IOP presents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.

Mechanism of action

Bimatoprost is believed to lower intraocular pressure (IOP) in humans by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Bimatoprost reduces the pressure in the eye by mimicking the action of a naturally-occuring prostaglandin. Prostaglandins are a group of chemicals found in many places in the body. In the eye, they increase the drainage of the aqueous humour out of the eyeball. Bimatoprost is a synthetic compound related to one of the natural prostaglandins, and works by increasing the drainage of aqueous humour out of the eyeball. Bimatoprost may also lower the rate of aqueous formation in the eye. Both these effects decrease the pressure within the eye.

TargetActionsOrganism
AProstaglandin F2-alpha receptor
agonist
Human
AProstaglandin E2 receptor EP1 subtype
agonist
Human
AProstaglandin E2 receptor EP3 subtype
agonist
Human
UAldo-keto reductase family 1 member C3Not AvailableHuman
Absorption

Systemically absorbed when administered to the eye.

Volume of distribution
  • 0.67 L/kg
Protein binding

Approximately 88% of bimatoprost is bound in human plasma.

Metabolism

Bimatoprost undergoes oxidation, N-deethylation and glucuronidation to form a variety of metabolites.

Route of elimination

Up to 67% of the administered dose was excreted in the urine while 25% of the dose was recovered in the feces.

Half life

Elimination half-life is approximately 45 minutes.

Clearance
  • 1.5 L/hr/kg [Healthy subjects receiving IV administration of 3.12 ug/kg]
Toxicity

In oral (by gavage) mouse and rat studies, doses up to 100 mg/kg/day did not produce any toxicity. This dose expressed as mg/m2 is at least 70 times higher than the accidental dose of one bottle of bimatoprost for a 10 kg child.

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

Interactions

Drug Interactions
DrugInteraction
AcebutololBimatoprost may increase the hypotensive activities of Acebutolol.
AceclofenacThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Acemetacin.
Acetylsalicylic acidThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Acetylsalicylic acid.
AlclofenacThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Alclofenac.
AliskirenBimatoprost may increase the hypotensive activities of Aliskiren.
AlminoprofenThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Alminoprofen.
AlprenololAlprenolol may increase the hypotensive activities of Bimatoprost.
AmbrisentanBimatoprost may increase the hypotensive activities of Ambrisentan.
AminophenazoneThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Aminophenazone.
Food Interactions
Not Available

References

Synthesis Reference

Jiang Xing Chen, "Process for the production of intermediates for making prostaglandin derivatives such as latanaprost, travaprost, and bimatoprost." U.S. Patent US20090287003, issued November 19, 2009.

US20090287003
General References
  1. Chen MJ, Cheng CY, Chen YC, Chou CK, Hsu WM: Effects of bimatoprost 0.03% on ocular hemodynamics in normal tension glaucoma. J Ocul Pharmacol Ther. 2006 Jun;22(3):188-93. [PubMed:16808680]
  2. Kruse P, Rieck P, Sherif Z, Liekfeld A: [Cystoid macular edema in a pseudophakic patient after several glaucoma procedures. Is local therapy with bimatoprost the reason?]. Klin Monbl Augenheilkd. 2006 Jun;223(6):534-7. [PubMed:16804825]
  3. Steinhauser SL: Decreased high-density lipoprotein serum levels associated with topical bimatoprost therapy. Optometry. 2006 Apr;77(4):177-9. [PubMed:16567279]
  4. Woodward DF, Krauss AH, Chen J, Lai RK, Spada CS, Burk RM, Andrews SW, Shi L, Liang Y, Kedzie KM, Chen R, Gil DW, Kharlamb A, Archeampong A, Ling J, Madhu C, Ni J, Rix P, Usansky J, Usansky H, Weber A, Welty D, Yang W, Tang-Liu DD, Garst ME, Brar B, Wheeler LA, Kaplan LJ: The pharmacology of bimatoprost (Lumigan). Surv Ophthalmol. 2001 May;45 Suppl 4:S337-45. [PubMed:11434936]
  5. Lim KS, Nau CB, O'Byrne MM, Hodge DO, Toris CB, McLaren JW, Johnson DH: Mechanism of action of bimatoprost, latanoprost, and travoprost in healthy subjects. A crossover study. Ophthalmology. 2008 May;115(5):790-795.e4. doi: 10.1016/j.ophtha.2007.07.002. [PubMed:18452763]
  6. Brubaker RF: Mechanism of action of bimatoprost (Lumigan). Surv Ophthalmol. 2001 May;45 Suppl 4:S347-51. [PubMed:11434937]
  7. Christiansen GA, Nau CB, McLaren JW, Johnson DH: Mechanism of ocular hypotensive action of bimatoprost (Lumigan) in patients with ocular hypertension or glaucoma. Ophthalmology. 2004 Sep;111(9):1658-62. [PubMed:15350319]
  8. Easthope SE, Perry CM: Topical bimatoprost: a review of its use in open-angle glaucoma and ocular hypertension. Drugs Aging. 2002;19(3):231-48. [PubMed:12027782]
  9. Patil AJ, Vajaranant TS, Edward DP: Bimatoprost - a review. Expert Opin Pharmacother. 2009 Nov;10(16):2759-68. doi: 10.1517/14656560903292649. [PubMed:19874254]
External Links
Human Metabolome Database
HMDB0015041
PubChem Compound
5311027
PubChem Substance
46505334
ChemSpider
4470565
BindingDB
220120
ChEBI
51230
ChEMBL
CHEMBL1200963
Therapeutic Targets Database
DAP001217
PharmGKB
PA164748867
IUPHAR
1958
Guide to Pharmacology
GtP Drug Page
HET
15M
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Bimatoprost
ATC Codes
S01EE03 — Bimatoprost
AHFS Codes
  • 52:40.28 — Prostaglandin Analogs
PDB Entries
2f38
FDA label
Download (24.4 KB)
MSDS
Download (19.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingTreatmentDermatochalasis1
0RecruitingTreatmentGraves Ophthalmopathy1
1TerminatedTreatmentAndrogenetic Alopecia / Hair Thinning1
1, 2CompletedTreatmentGlaucoma / Ocular Hypertension1
1, 2CompletedTreatmentOcular Hypertension / Open-angle Glaucoma (OAG)2
2CompletedTreatmentAndrogenetic Alopecia / Male Pattern Hair Loss1
2CompletedTreatmentEyelash Hypotrichosis1
2CompletedTreatmentGlaucoma, Primary Open Angle (POAG) / Ocular Hypertension3
2CompletedTreatmentGlaucoma / Ocular Hypertension3
2CompletedTreatmentOcular Hypertension / Open-angle Glaucoma (OAG)3
2RecruitingPreventionHeadache Disorders / Migraine Disorders1
2, 3CompletedTreatmentOcular Hypertension1
3CompletedTreatmentEyebrow Hypotrichosis1
3CompletedTreatmentEyelash Hypotrichosis2
3CompletedTreatmentEyelashes1
3CompletedTreatmentGlaucoma1
3CompletedTreatmentGlaucoma / Ocular Hypertension2
3CompletedTreatmentHypotrichosis1
3CompletedTreatmentHypotrichosis / Madarosis1
3CompletedTreatmentIdiopathic Eyelash Hypotrichosis1
3CompletedTreatmentThyroid Associated Ophthalmopathy1
3RecruitingPreventionGlaucoma1
4CompletedNot AvailableGlaucoma1
4CompletedNot AvailableGlaucoma, Primary Open Angle (POAG) / Ocular Hypertension2
4CompletedTreatmentAlopecia Areata (AA) / Eyelash Hypotrichosis1
4CompletedTreatmentAnterior Uveitis (AU) / Cystoid Macular Edema1
4CompletedTreatmentApplication Site Pigmentation Changes / Glaucoma1
4CompletedTreatmentCataracts1
4CompletedTreatmentCrow's Feet Lines / Facial Rhytides / Glabellar Lines / Nasolabial Folds1
4CompletedTreatmentEndocrine ophthalmopathy1
4CompletedTreatmentEyelash Hypotrichosis1
4CompletedTreatmentGlaucoma, Primary Open Angle (POAG) / Ocular Hypertension1
4CompletedTreatmentGlaucoma / Intraocular Pressure / Ocular Hypertension1
4CompletedTreatmentGlaucoma / Ocular Hypertension10
4CompletedTreatmentGlaucoma / Ocular Hypertension / Open-angle Glaucoma (OAG)1
4CompletedTreatmentHypotrichosis4
4CompletedTreatmentNormal Tension Glaucoma / Open-angle Glaucoma (OAG)1
4CompletedTreatmentOcular Hypertension1
4CompletedTreatmentOcular Hypertension / Open Angle Glaucoma (OAG)2
4CompletedTreatmentOcular Hypertension / Open-angle Glaucoma (OAG)6
4CompletedTreatmentOpen-angle Glaucoma (OAG)1
4RecruitingTreatmentGlaucoma1
4RecruitingTreatmentGlaucoma, Primary Open Angle (POAG) / Ocular Hypertension1
4RecruitingTreatmentGlaucoma / Ocular Hypertension1
4WithdrawnPreventionGlaucoma / Ocular Hypertension / Thyroid Eye Disease1
4WithdrawnTreatmentRepigmentation / Vitiligo1
Not AvailableActive Not RecruitingTreatmentIntraocular Pressure / Nail Growth Cessation1
Not AvailableCompletedNot AvailableEyelash Hypotrichosis2
Not AvailableCompletedNot AvailableOcular Hypertension / Open-angle Glaucoma (OAG)8
Not AvailableCompletedTreatmentAlopecia Areata (AA)1
Not AvailableCompletedTreatmentHypertrichosis1
Not AvailableCompletedTreatmentOcular Hypertension / Open-angle Glaucoma (OAG)1
Not AvailableRecruitingTreatmentGlaucoma1
Not AvailableUnknown StatusTreatmentGlaucoma, Angle-Closure1
Not AvailableUnknown StatusTreatmentOcular Hypertension / Primary Glaucoma1
Not AvailableWithdrawnSupportive CareCancer, Breast / Hair Thinning1

Pharmacoeconomics

Manufacturers
  • Allergan inc
Packagers
  • Allergan Inc.
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
SolutionOphthalmic0.03 %
SolutionTopical3 ug/1mL
SolutionTopical0.03 %
SolutionOphthalmic0.3 mg/1mL
Solution / dropsOphthalmic0.1 mg/1mL
Solution / dropsOphthalmic0.3 mg/1mL
SolutionOphthalmic0.01 %
Prices
Unit descriptionCostUnit
Lumigan .03% 7.5ml Bottle279.56USD bottle
Lumigan .03% 5ml Bottle171.4USD bottle
Lumigan .03% 2.5ml Bottle91.16USD bottle
Lumigan 0.03% eye drops44.82USD ml
Latisse 0.03% eyelash solution36.0USD ml
Lumigan 0.03 % Solution12.18USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6403649No2002-06-112012-09-21Us
CA2585691No2009-05-192026-03-14Canada
CA2144967No2003-11-112013-09-09Canada
US8299118No2012-10-302025-03-16Us
US8309605No2012-11-132025-03-16Us
US8338479No2012-12-252025-03-16Us
US8586630No2013-11-192025-03-16Us
US8524777No2013-09-032025-03-16Us
US8772338No2014-07-082025-03-16Us
US9155716No2015-10-132025-03-16Us
US9241918No2016-01-262025-03-16Us
US7851504No2010-12-142027-06-13Us
US8933120No2015-01-132025-03-16Us
US8933127No2015-01-132025-03-16Us
US8278353No2012-10-022025-03-16Us
US8906962No2014-12-092021-01-31Us
US8038988No2011-10-182023-08-25Us
US8101161No2012-01-242024-05-25Us
US8263054No2012-09-112023-01-15Us
US8632760No2014-01-212023-01-15Us
US8758733No2014-06-242023-01-15Us
US8926953No2015-01-062023-01-15Us
US8541466No2013-09-242021-01-31Us
US7388029No2008-06-172022-01-21Us
US7351404No2008-04-012024-05-25Us
US9216183No2015-12-222023-01-15Us
US9226931No2016-01-052023-01-15Us
US8986715No2015-03-242023-01-15Us
US9579270No2017-02-282021-01-31Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySlightly solubleNot Available
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0187 mg/mLALOGPS
logP3.41ALOGPS
logP2.63ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)14.35ChemAxon
pKa (Strongest Basic)-0.23ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area89.79 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity122.83 m3·mol-1ChemAxon
Polarizability48.99 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9975
Blood Brain Barrier+0.825
Caco-2 permeable-0.5699
P-glycoprotein substrateSubstrate0.5541
P-glycoprotein inhibitor INon-inhibitor0.8671
P-glycoprotein inhibitor IINon-inhibitor0.8616
Renal organic cation transporterNon-inhibitor0.8078
CYP450 2C9 substrateNon-substrate0.7703
CYP450 2D6 substrateNon-substrate0.7406
CYP450 3A4 substrateSubstrate0.552
CYP450 1A2 substrateNon-inhibitor0.6764
CYP450 2C9 inhibitorNon-inhibitor0.7695
CYP450 2D6 inhibitorNon-inhibitor0.6384
CYP450 2C19 inhibitorNon-inhibitor0.7632
CYP450 3A4 inhibitorNon-inhibitor0.757
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7049
Ames testNon AMES toxic0.7646
CarcinogenicityNon-carcinogens0.9257
BiodegradationNot ready biodegradable0.6415
Rat acute toxicity2.1085 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9251
hERG inhibition (predictor II)Non-inhibitor0.7822
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as prostaglandins and related compounds. These are unsaturated carboxylic acids consisting of a 20 carbon skeleton that also contains a five member ring, and are based upon the fatty acid arachidonic acid.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Fatty Acyls
Sub Class
Eicosanoids
Direct Parent
Prostaglandins and related compounds
Alternative Parents
N-acyl amines / Cyclopentanols / Benzene and substituted derivatives / Secondary carboxylic acid amides / Cyclic alcohols and derivatives / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Prostaglandin skeleton / Monocyclic benzene moiety / Cyclopentanol / Fatty amide / Benzenoid / N-acyl-amine / Cyclic alcohol / Carboxamide group / Secondary carboxylic acid amide / Secondary alcohol
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
monocarboxylic acid amide (CHEBI:51230)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Prostaglandin f receptor activity
Specific Function
Receptor for prostaglandin F2-alpha (PGF2-alpha). The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. Initiates luteolysis...
Gene Name
PTGFR
Uniprot ID
P43088
Uniprot Name
Prostaglandin F2-alpha receptor
Molecular Weight
40054.1 Da
References
  1. Sharif NA, Williams GW, Kelly CR: Bimatoprost and its free acid are prostaglandin FP receptor agonists. Eur J Pharmacol. 2001 Dec 7;432(2-3):211-3. [PubMed:11740958]
  2. Sharif NA, Kelly CR, Crider JY: Agonist activity of bimatoprost, travoprost, latanoprost, unoprostone isopropyl ester and other prostaglandin analogs at the cloned human ciliary body FP prostaglandin receptor. J Ocul Pharmacol Ther. 2002 Aug;18(4):313-24. [PubMed:12222762]
  3. Sharif NA, Kelly CR, Crider JY, Williams GW, Xu SX: Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cells. J Ocul Pharmacol Ther. 2003 Dec;19(6):501-15. [PubMed:14733708]
  4. Lim KS, Nau CB, O'Byrne MM, Hodge DO, Toris CB, McLaren JW, Johnson DH: Mechanism of action of bimatoprost, latanoprost, and travoprost in healthy subjects. A crossover study. Ophthalmology. 2008 May;115(5):790-795.e4. doi: 10.1016/j.ophtha.2007.07.002. [PubMed:18452763]
  5. Mintz EE: Group supervision: an experiential approach. Int J Group Psychother. 1978 Oct;28(4):467-9. [PubMed:689791]
  6. Neacsu AM: [Receptors involved in the mechanism of action of topical prostaglandines]. Oftalmologia. 2009;53(2):3-7. [PubMed:19697832]
  7. Wan Z, Woodward DF, Cornell CL, Fliri HG, Martos JL, Pettit SN, Wang JW, Kharlamb AB, Wheeler LA, Garst ME, Landsverk KJ, Struble CS, Stamer WD: Bimatoprost, prostamide activity, and conventional drainage. Invest Ophthalmol Vis Sci. 2007 Sep;48(9):4107-15. [PubMed:17724194]
  8. 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
Yes
Actions
Agonist
General Function
Prostaglandin e receptor activity
Specific Function
Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an importa...
Gene Name
PTGER1
Uniprot ID
P34995
Uniprot Name
Prostaglandin E2 receptor EP1 subtype
Molecular Weight
41800.655 Da
References
  1. Sharif NA, Kelly CR, Crider JY, Williams GW, Xu SX: Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cells. J Ocul Pharmacol Ther. 2003 Dec;19(6):501-15. [PubMed:14733708]
  2. Ota T, Aihara M, Saeki T, Narumiya S, Araie M: The effects of prostaglandin analogues on prostanoid EP1, EP2, and EP3 receptor-deficient mice. Invest Ophthalmol Vis Sci. 2006 Aug;47(8):3395-9. [PubMed:16877408]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Rna polymerase ii transcription factor activity, ligand-activated sequence-specific dna binding
Specific Function
Receptor for prostaglandin E2 (PGE2); the EP3 receptor may be involved in inhibition of gastric acid secretion, modulation of neurotransmitter release in central and peripheral neurons, inhibition ...
Gene Name
PTGER3
Uniprot ID
P43115
Uniprot Name
Prostaglandin E2 receptor EP3 subtype
Molecular Weight
43309.335 Da
References
  1. Sharif NA, Kelly CR, Crider JY, Williams GW, Xu SX: Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cells. J Ocul Pharmacol Ther. 2003 Dec;19(6):501-15. [PubMed:14733708]
  2. Gabelt BT, Hennes EA, Bendel MA, Constant CE, Okka M, Kaufman PL: Prostaglandin subtype-selective and non-selective IOP-lowering comparison in monkeys. J Ocul Pharmacol Ther. 2009 Feb;25(1):1-8. doi: 10.1089/jop.2008.0089. [PubMed:19232013]
  3. Ota T, Aihara M, Saeki T, Narumiya S, Araie M: The effects of prostaglandin analogues on prostanoid EP1, EP2, and EP3 receptor-deficient mice. Invest Ophthalmol Vis Sci. 2006 Aug;47(8):3395-9. [PubMed:16877408]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
Specific Function
Catalyzes the conversion of aldehydes and ketones to alcohols. Catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2....
Gene Name
AKR1C3
Uniprot ID
P42330
Uniprot Name
Aldo-keto reductase family 1 member C3
Molecular Weight
36852.89 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]

Drug created on June 13, 2005 07:24 / Updated on November 16, 2018 11:14