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Identification
NameOlopatadine
Accession NumberDB00768  (APRD00310)
TypeSmall Molecule
GroupsApproved
Description

Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.

Structure
Thumb
Synonyms
Olopatadin
Olopatadina
Olopatadine
Olopatadinum
Opatanol
External Identifiers
  • ALO 4943 A
  • KW 4679
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Olopatadine 0.1%solution0.1 %ophthalmicActavis Pharma Company2013-12-06Not applicableCanada
Act Olopatadine 0.2%solution0.2 %ophthalmicActavis Pharma Company2014-02-20Not applicableCanada
Mint-olopatadinesolution0.1 %ophthalmicMint Pharmaceuticals Inc2014-07-29Not applicableCanada
Olopatadine Hydrochloridespray, metered665 ug/100uLnasalFalcon Pharmaceuticals, Ltd.2012-06-30Not applicableUs
Olopatadine Hydrochloridesolution/ drops1 mg/mLophthalmicSandoz Inc.2015-09-15Not applicableUs
Olopatadine Hydrochloride Nasalspray665 ug/1nasalPerrigo New York Inc2015-04-01Not applicableUs
Patadaysolution/ drops2 mg/mLophthalmicPhysicians Total Care, Inc.2011-01-03Not applicableUs
Patadaysolution0.2 %ophthalmicAlcon Canada Inc2011-04-14Not applicableCanada
Patadaysolution/ drops2 mg/mLophthalmicLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-04-03Not applicableUs
Patadaysolution/ drops2 mg/mLophthalmicAlcon Laboratories, Inc.2007-02-15Not applicableUs
Patanasespray, metered665 ug/1nasalPhysicians Total Care, Inc.2009-07-13Not applicableUs
Patanasespray, metered600 ug/1nasalAlcon Laboratories, Inc.2008-04-28Not applicableUs
Patanasespray, metered665 ug/1nasalClinical Solutions Wholesale2008-04-28Not applicableUs
Patanolsolution/ drops1 mg/mLophthalmicAlcon Laboratories, Inc.1997-02-17Not applicableUs
Patanolsolution/ drops1 mg/mLophthalmicPhysicians Total Care, Inc.2002-05-08Not applicableUs
Patanol Ophthalmic Solutionliquid0.1 %ophthalmicAlcon Canada Inc1998-02-09Not applicableCanada
Pazeosolution7 mg/mLophthalmicAlcon Laboratories, Inc.2015-01-29Not applicableUs
Sandoz Olopatadinesolution0.1 %ophthalmicSandoz Canada Incorporated2013-02-04Not applicableCanada
Sandoz Olopatadine 0.2%solution0.2 %ophthalmicSandoz Canada Incorporated2014-02-24Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-olopatadinesolution0.2 %ophthalmicApotex Inc2014-04-10Not applicableCanada
Apo-olopatadinesolution0.1 %ophthalmicApotex Inc2013-07-26Not applicableCanada
Olopatadine Hydrochloridesolution/ drops1.11 mg/mLophthalmicNovel Laboratories, Inc.2015-12-07Not applicableUs
Olopatadine Hydrochloridesolution/ drops1 mg/mLophthalmicAurobindo Pharma Limited2015-12-18Not applicableUs
Olopatadine Hydrochloridesolution/ drops1 mg/mLophthalmicRising Pharmaceuticals, Inc.2015-12-07Not applicableUs
Olopatadine Hydrochloridespray, metered665 ug/1nasalApotex Corp.2014-10-27Not applicableUs
Olopatadine Hydrochloridesolution/ drops1 mg/mLophthalmicApotex Corp.2015-12-07Not applicableUs
Olopatadine Hydrochloridesolution/ drops1 mg/mLophthalmicAlvogen Inc.2015-12-08Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlchekApex
AlerchekIndoco
AllelockDae Woong
OpatanolAlcon
Patanol SAlcon
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Olopatadine Hydrochloride
Thumb
  • InChI Key: HVRLZEKDTUEKQH-NOILCQHBSA-N
  • Monoisotopic Mass: 373.144471346
  • Average Mass: 373.873
DBSALT000685
Categories
UNIID27V6190PM
CAS number113806-05-6
WeightAverage: 337.4122
Monoisotopic: 337.167793607
Chemical FormulaC21H23NO3
InChI KeyInChIKey=JBIMVDZLSHOPLA-LSCVHKIXSA-N
InChI
InChI=1S/C21H23NO3/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24)/b18-8-
IUPAC Name
2-[(2Z)-2-[3-(dimethylamino)propylidene]-9-oxatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3(8),4,6,11,13-hexaen-5-yl]acetic acid
SMILES
CN(C)CC\C=C1\C2=CC=CC=C2COC2=C1C=C(CC(O)=O)C=C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzoxepines. These are compounds containing a dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxepines
Sub ClassDibenzoxepines
Direct ParentDibenzoxepines
Alternative Parents
Substituents
  • Dibenzoxepine
  • Alkyl aryl ether
  • Benzenoid
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of ocular itching associated with allergic conjunctivitis.
PharmacodynamicsUsed to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.
Mechanism of actionOlopatadine is a selective histamine H1 antagonist that binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors.
Related Articles
AbsorptionOphthalmic use of olopatadine usually does not produce measurable plasma concentrations.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

The mono-desmethyl and the N-oxide metabolites have been detected at low concentrations in the urine.

SubstrateEnzymesProduct
Olopatadine
Not Available
Mono-desmethyl olopatadineDetails
Olopatadine
Not Available
Olopatadine n-oxideDetails
Route of eliminationElimination was predominantly through renal excretion.
Half life3 hours
ClearanceNot Available
ToxicityNot Available
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+0.9747
Blood Brain Barrier+0.6925
Caco-2 permeable+0.7249
P-glycoprotein substrateSubstrate0.8607
P-glycoprotein inhibitor IInhibitor0.5948
P-glycoprotein inhibitor IINon-inhibitor0.8196
Renal organic cation transporterInhibitor0.5413
CYP450 2C9 substrateNon-substrate0.7691
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7242
CYP450 1A2 substrateInhibitor0.7906
CYP450 2C9 inhibitorNon-inhibitor0.8316
CYP450 2D6 inhibitorInhibitor0.6567
CYP450 2C19 inhibitorNon-inhibitor0.8466
CYP450 3A4 inhibitorNon-inhibitor0.8222
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8676
Ames testNon AMES toxic0.8032
CarcinogenicityNon-carcinogens0.8499
BiodegradationNot ready biodegradable0.6088
Rat acute toxicity2.7626 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8082
hERG inhibition (predictor II)Inhibitor0.5
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Alcon inc
  • Alcon laboratories inc
  • Alcon Laboratories, Inc.
Packagers
Dosage forms
FormRouteStrength
Solutionophthalmic0.1 %
Solution/ dropsophthalmic1.11 mg/mL
Spray, meterednasal665 ug/100uL
Spraynasal665 ug/1
Solutionophthalmic0.2 %
Solution/ dropsophthalmic2 mg/mL
Spray, meterednasal600 ug/1
Spray, meterednasal665 ug/1
Solution/ dropsophthalmic1 mg/mL
Liquidophthalmic0.1 %
Solutionophthalmic7 mg/mL
Prices
Unit descriptionCostUnit
Patanol 0.1% Solution 5ml Bottle111.2USD bottle
Pataday 0.2% eye drops52.98USD ml
Patanol 0.1% eye drops21.38USD ml
Patanase 0.6% nasal spray3.83USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1337603 No1995-11-212012-11-21Canada
CA2195094 No2002-02-262016-05-03Canada
US5116863 No1993-12-182010-12-18Us
US5641805 Yes1995-12-062015-12-06Us
US6995186 Yes2004-05-122024-05-12Us
US7402609 Yes2002-12-192022-12-19Us
US7977376 Yes2003-08-022023-08-02Us
US8399508 Yes2003-03-172023-03-17Us
US8791154 No2012-05-192032-05-19Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point248 °CNot Available
water solubilitySolubleNot Available
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0313 mg/mLALOGPS
logP3.99ALOGPS
logP0.75ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)3.78ChemAxon
pKa (Strongest Basic)9.76ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area49.77 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity109.55 m3·mol-1ChemAxon
Polarizability37.44 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Thomas Bader, Hans-Ulrich Bichsel, Bruno Gilomen, Imelda Meyer-Wilmes, Mark Sundermeier, “Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof.” U.S. Patent US20070232814, issued October 04, 2007.

US20070232814
General References
  1. Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A: Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol. 2002 Apr;88(4):379-97. [PubMed:12046981 ]
  2. Yanni JM, Stephens DJ, Miller ST, Weimer LK, Graff G, Parnell D, Lang LS, Spellman JM, Brady MT, Gamache DA: The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther. 1996 Winter;12(4):389-400. [PubMed:8951675 ]
  3. Ohmori K, Hasegawa K, Tamura T, Miyake K, Matsubara M, Masaki S, Karasawa A, Urayama N, Horikoshi K, Kajita J, Hasegawa M, Taniguchi K, Komada T, Kawamoto Y: Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittelforschung. 2004;54(12):809-29. [PubMed:15646365 ]
  4. Ohmori K, Ikemura T, Kobayashi H, Mukouyama A: [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]. Nihon Yakurigaku Zasshi. 2001 Jul;118(1):51-8. [PubMed:11496828 ]
  5. Kaliner MA, Oppenheimer J, Farrar JR: Comprehensive review of olopatadine: the molecule and its clinical entities. Allergy Asthma Proc. 2010 Mar-Apr;31(2):112-9. doi: 10.2500/aap.2010.31.3317. [PubMed:20406593 ]
External Links
ATC CodesR01AC08S01GX09
AHFS Codes
  • 04:00.00
PDB EntriesNot Available
FDA labelDownload (114 KB)
MSDSDownload (57.6 KB)
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Olopatadine.
AmphetamineAmphetamine may decrease the sedative activities of Olopatadine.
AzelastineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Olopatadine.
Benzylpenicilloyl PolylysineOlopatadine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Olopatadine.
Botulinum Toxin Type AOlopatadine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BOlopatadine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
BuprenorphineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CathinoneCathinone may decrease the sedative activities of Olopatadine.
Cimetropium BromideOlopatadine may increase the anticholinergic activities of Cimetropium Bromide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
EluxadolineOlopatadine may increase the activities of Eluxadoline.
EthanolOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Olopatadine is combined with Glucagon recombinant.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Olopatadine.
HydrocodoneOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Olopatadine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Olopatadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Olopatadine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
MethotrimeprazineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineOlopatadine may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Olopatadine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
MirabegronThe risk or severity of adverse effects can be increased when Olopatadine is combined with Mirabegron.
MirtazapineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MorphineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
OrphenadrineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
Potassium ChlorideOlopatadine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleOlopatadine may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Olopatadine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Olopatadine.
RamosetronOlopatadine may increase the activities of Ramosetron.
RopiniroleOlopatadine may increase the sedative activities of Ropinirole.
RotigotineOlopatadine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Olopatadine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Olopatadine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Olopatadine.
SuvorexantOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Olopatadine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.
ThalidomideOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiotropiumOlopatadine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Olopatadine is combined with Topiramate.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Olopatadine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Olopatadine.
ZolpidemOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Tamura T, Masaki S, Ohmori K, Karasawa A: Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology. 2005 Dec;75(1):45-52. Epub 2005 Jun 7. [PubMed:15942272 ]
  2. Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A: Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol. 2002 Apr;88(4):379-97. [PubMed:12046981 ]
  3. Yanni JM, Stephens DJ, Miller ST, Weimer LK, Graff G, Parnell D, Lang LS, Spellman JM, Brady MT, Gamache DA: The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther. 1996 Winter;12(4):389-400. [PubMed:8951675 ]
  4. Ohmori K, Hasegawa K, Tamura T, Miyake K, Matsubara M, Masaki S, Karasawa A, Urayama N, Horikoshi K, Kajita J, Hasegawa M, Taniguchi K, Komada T, Kawamoto Y: Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittelforschung. 2004;54(12):809-29. [PubMed:15646365 ]
  5. Ohmori K, Ikemura T, Kobayashi H, Mukouyama A: [Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]. Nihon Yakurigaku Zasshi. 2001 Jul;118(1):51-8. [PubMed:11496828 ]
  6. Roland PS, Ryan MW, Wall GM: Olopatadine nasal spray for the treatment of seasonal allergic rhinitis in patients aged 6 years and older. Expert Opin Pharmacother. 2010 Jun;11(9):1559-67. doi: 10.1517/14656566.2010.485609. [PubMed:20482305 ]
  7. Kaliner MA, Oppenheimer J, Farrar JR: Comprehensive review of olopatadine: the molecule and its clinical entities. Allergy Asthma Proc. 2010 Mar-Apr;31(2):112-9. doi: 10.2500/aap.2010.31.3317. [PubMed:20406593 ]
  8. Roland PS, Marple BF, Wall GM: Olopatadine nasal spray for the treatment of allergic rhinitis. Expert Rev Clin Immunol. 2010 Mar;6(2):197-204. [PubMed:20402382 ]
  9. 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:
S100 protein binding
Specific Function:
Weakly binds calcium but binds zinc very tightly-distinct binding sites with different affinities exist for both ions on each monomer. Physiological concentrations of potassium ion antagonize the binding of both divalent cations, especially affecting high-affinity calcium-binding sites. May mediate calcium-dependent regulation on many physiological processes by interacting with other proteins, ...
Gene Name:
S100A1
Uniprot ID:
P23297
Molecular Weight:
10545.755 Da
References
  1. Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [PubMed:11944917 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
S100A12 is a calcium-, zinc- and copper-binding protein which plays a prominent role in the regulation of inflammatory processes and immune response. Its proinflammatory activity involves recruitment of leukocytes, promotion of cytokine and chemokine production, and regulation of leukocyte adhesion and migration. Acts as an alarmin or a danger associated molecular pattern (DAMP) molecule and st...
Gene Name:
S100A12
Uniprot ID:
P80511
Molecular Weight:
10574.975 Da
References
  1. Kishimoto K, Kaneko S, Ohmori K, Tamura T, Hasegawa K: Olopatadine suppresses the migration of THP-1 monocytes induced by S100A12 protein. Mediators Inflamm. 2006;2006(1):42726. [PubMed:16864903 ]
  2. Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [PubMed:11944917 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
General Function:
Zinc ion binding
Specific Function:
Weakly binds calcium but binds zinc very tightly-distinct binding sites with different affinities exist for both ions on each monomer. Physiological concentrations of potassium ion antagonize the binding of both divalent cations, especially affecting high-affinity calcium-binding sites. Binds to and initiates the activation of STK38 by releasing autoinhibitory intramolecular interactions within...
Gene Name:
S100B
Uniprot ID:
P04271
Molecular Weight:
10712.985 Da
References
  1. Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [PubMed:11944917 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
General Function:
Zinc ion binding
Specific Function:
Plays a role in the export of proteins that lack a signal peptide and are secreted by an alternative pathway. Binds two calcium ions per subunit. Binds one copper ion. Binding of one copper ion does not interfere with calcium binding. Required for the copper-dependent stress-induced export of IL1A and FGF1. The calcium-free protein binds to lipid vesicles containing phosphatidylserine, but not ...
Gene Name:
S100A13
Uniprot ID:
Q99584
Molecular Weight:
11471.095 Da
References
  1. Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [PubMed:11944917 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Identical protein binding
Specific Function:
May function as calcium sensor and modulator, contributing to cellular calcium signaling. May function by interacting with other proteins, such as TPR-containing proteins, and indirectly play a role in many physiological processes. May also play a role in suppressing tumor cell growth.
Gene Name:
S100A2
Uniprot ID:
P29034
Molecular Weight:
11116.695 Da
References
  1. Okada M, Tokumitsu H, Kubota Y, Kobayashi R: Interaction of S100 proteins with the antiallergic drugs, olopatadine, amlexanox, and cromolyn: identification of putative drug binding sites on S100A1 protein. Biochem Biophys Res Commun. 2002 Apr 12;292(4):1023-30. [PubMed:11944917 ]

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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 ]
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Drug created on June 13, 2005 07:24 / Updated on May 31, 2016 03:27