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Identification
NamePilocarpine
Accession NumberDB01085  (APRD00382)
TypeSmall Molecule
GroupsApproved
Description

A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. [PubChem]

Structure
Thumb
Synonyms
(3S-cis)-3-Ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone
(3S,4R)-3-Ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-2(3H)-furanone
Pilocarpine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Diocarpine 1% Solutionsolution1 %ophthalmicDioptic Pharmaceuticals Inc1994-12-31Not applicableCanada
Diocarpine 2% Solutionliquid2 %ophthalmicDioptic Pharmaceuticals Inc1994-12-31Not applicableCanada
Diocarpine 4% Solutionliquid4 %ophthalmicDioptic Pharmaceuticals Inc1994-12-31Not applicableCanada
Isopto Carpinesolution/ drops40 mg/mLophthalmicAlcon Laboratories, Inc.1974-01-01Not applicableUs
Isopto Carpinesolution/ drops20 mg/mLophthalmicAlcon Laboratories, Inc.1974-01-01Not applicableUs
Isopto Carpinesolution/ drops10 mg/mLophthalmicAlcon Laboratories, Inc.1974-01-01Not applicableUs
Isopto Carpine 0.5%liquid0.5 %ophthalmicAlcon Canada Inc1951-12-312002-04-16Canada
Isopto Carpine Liq 1%liquid10 mgophthalmicAlcon Canada Inc1959-12-31Not applicableCanada
Isopto Carpine Liq 2%liquid20 mgophthalmicAlcon Canada Inc1959-12-31Not applicableCanada
Isopto Carpine Liq 4%liquid40 mgophthalmicAlcon Canada Inc1959-12-31Not applicableCanada
Isopto Carpine Liq 6%liquid60 gophthalmicAlcon Canada Inc1959-12-312001-08-14Canada
Minims Pilocarpine Nitrate 2%drops2 %ophthalmicValeant Canada Lp Valeant Canada S.E.C.1995-12-31Not applicableCanada
Minims Pilocarpine Nitrate 4%drops4 %ophthalmicChauvin Pharmaceuticals Limited1995-12-312009-02-04Canada
Miocarpine Oph Soln 1%drops1 %ophthalmicIolab Pharmaceuticals1988-12-311997-07-23Canada
Miocarpine Oph Soln 2%drops2 %ophthalmicIolab Pharmaceuticals1988-12-311996-09-09Canada
Miocarpine Oph Soln 4%drops4 %ophthalmicIolab Pharmaceuticals1988-12-311996-09-09Canada
Miocarpine Oph Soln 6%drops6 %ophthalmicIolab Pharmaceuticals1988-12-311997-07-23Canada
Miocarpine Ophthalmic Solution 1%drops1 %ophthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1997-02-112001-08-27Canada
Miocarpine Ophthalmic Solution 2%drops2 %ophthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1996-12-312001-10-09Canada
Miocarpine Ophthalmic Solution 4%drops4 %ophthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1996-12-312002-07-09Canada
Miocarpine Ophthalmic Solution 6%drops6 %ophthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1997-02-112002-02-01Canada
Ocusert Pilo 20implant5 mgintraocularAlza Pharms Division Of Alza Corp1975-12-311997-08-18Canada
Ocusert Pilo 40implant11 mgintraocularAlza Pharms Division Of Alza Corp1975-12-311997-08-18Canada
Odan-pilocarpinesolution4 %ophthalmicOdan Laboratories Ltd1991-12-31Not applicableCanada
Odan-pilocarpinesolution2 %ophthalmicOdan Laboratories Ltd1992-12-31Not applicableCanada
Odan-pilocarpinesolution1 %ophthalmicOdan Laboratories Ltd1991-12-31Not applicableCanada
Pilocarpine 1%solution1 %ophthalmicIvax Pharmaceuticals Incorporated1996-11-132015-10-26Canada
Pilocarpine 2%solution2 %ophthalmicIvax Pharmaceuticals Incorporated1996-11-082015-10-26Canada
Pilocarpine 4%solution4 %ophthalmicIvax Pharmaceuticals Incorporated1996-11-082015-10-26Canada
Pilocarpine 6%solution6 %ophthalmicIvax Pharmaceuticals Incorporated1997-01-302015-10-26Canada
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralActavis Pharma, Inc.2011-09-13Not applicableUs
Pilocarpine Hydrochloridesolution40 mg/mLophthalmicFalcon Pharmaceuticals, Ltd.1996-02-21Not applicableUs
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralCarilion Materials Management2011-09-13Not applicableUs
Pilocarpine Hydrochloridesolution20 mg/mLophthalmicFalcon Pharmaceuticals, Ltd.1996-02-21Not applicableUs
Pilocarpine Hydrochloridesolution10 mg/mLophthalmicFalcon Pharmaceuticals, Ltd.1996-02-21Not applicableUs
Pilocarpine Hydrochloridesolution40 mg/1ophthalmicREMEDYREPACK INC.2013-04-152016-04-05Us
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralAmerican Health Packaging2015-09-01Not applicableUs
Pilocarpine Hydrochloridesolution/ drops10 mg/mLconjunctivalRebel Distributors Corp2010-06-22Not applicableUs
Pilocarpine Hydrochloridetablet, film coated7.5 mg/1oralActavis Pharma, Inc.2011-09-13Not applicableUs
Pilocarpine Hydrochloride 1% - Liq Ophliquid1 %ophthalmicRivex Ophthalmics Inc.1997-05-072003-07-28Canada
Pilocarpine Hydrochloride 2% - Liq Ophliquid2 %ophthalmicRivex Ophthalmics Inc.1997-05-072003-07-28Canada
Pilocarpine Hydrochloride 4% - Liq Ophliquid4 %ophthalmicRivex Ophthalmics Inc.1997-05-072003-07-28Canada
Pilocarpine Hydrochloride Ophthalmic Solution 1% USPliquid1 %ophthalmicTechnilab Pharma Inc.1997-05-292004-08-03Canada
Pilocarpine Hydrochloride Ophthalmic Solution 2% USPliquid2 %ophthalmicTechnilab Pharma Inc.1997-05-292004-08-03Canada
Pilocarpine Hydrochloride Ophthalmic Solution 4% USPliquid4 %ophthalmicTechnilab Pharma Inc.1997-05-292004-08-03Canada
Pilocarpine Hydrochloride Tablets, USPtablet5 mgoralSterimax Inc2013-03-15Not applicableCanada
Pilopine Hs 4%gel4 %ophthalmicAlcon Canada Inc1985-12-312012-10-03Canada
PMS-pilocarpine 0.5%liquid5 mgophthalmicPharmascience IncNot applicableNot applicableCanada
PMS-pilocarpine 1%liquid10 mgophthalmicPharmascience IncNot applicableNot applicableCanada
PMS-pilocarpine 2%liquid20 mgophthalmicPharmascience IncNot applicableNot applicableCanada
PMS-pilocarpine 4%liquid40 mgophthalmicPharmascience IncNot applicableNot applicableCanada
PMS-pilocarpine 6%liquid60 mgophthalmicPharmascience IncNot applicableNot applicableCanada
R.O. -carpine 1%liquid1 %ophthalmicRichmond Pharmaceuticals Inc.1992-12-311997-08-11Canada
R.O.-carpine 2%liquid2 %ophthalmicRichmond Pharmaceuticals Inc.1992-12-311997-08-11Canada
R.O.-carpine 4%liquid4 %ophthalmicRichmond Pharmaceuticals Inc.1992-12-311997-08-11Canada
Salagentablet, film coated7.5 mg/1oralEisai Inc.1994-03-22Not applicableUs
Salagentablet, film coated5 mg/1oralEisai Inc.1994-03-22Not applicableUs
Salagen Tabletstablet5 mgoralPfizer Canada Inc1997-04-01Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pilocarpine Hydrochloridetablet5 mg/1oralRoxane Laboratories, Inc2004-12-222016-03-11Us
Pilocarpine Hydrochloridetablet, film coated7.5 mg/1oralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Pilocarpine Hydrochloridetablet, film coated7.5 mg/1oralLannett Company, Inc.2009-08-10Not applicableUs
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralImpax Generics2007-05-01Not applicableUs
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralLannett Company, Inc.2006-01-31Not applicableUs
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralCore Pharma, Llc2004-11-162016-04-05Us
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralKAISER FOUNDATION HOSPITALS2014-05-29Not applicableUs
Pilocarpine Hydrochloridetablet, film coated5 mg/1oralPhysicians Total Care, Inc.2011-07-21Not applicableUs
Pilocarpine Hydrochloridetablet, film coated7.5 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2007-05-012016-04-14Us
Pilocarpine Hydrochloridetablet5 mg/1oralRebel Distributors Corp2006-03-31Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DiocarpineNot Available
MiocarpineNot Available
PilostatNot Available
PiloviscNot Available
TimpiloNot Available
Brand mixtures
NameLabellerIngredients
Betoptic/piloAlcon Canada Inc
E-pilo 1 Ophthalmic SolutionCiba Vision Canada Inc
E-pilo 2 Ophthalmic SolutionCiba Vision Canada Inc
E-pilo 4 Ophthalmic SolutionCiba Vision Canada Inc
E-pilo 6 Ophthalmic SolutionCiba Vision Canada Inc
E-pilo-1 Oph SolnIolab Pharmaceuticals
E-pilo-2 Oph SolnIolab Pharmaceuticals
E-pilo-4 Oph SolnIolab Pharmaceuticals
E-pilo-6 Oph SolnIolab Pharmaceuticals
Timpilo 2Merck Canada Inc
Timpilo 4Merck Canada Inc
Salts
Name/CASStructureProperties
Pilocarpine hydrochloride
54-71-7
Thumb
  • InChI Key: RNAICSBVACLLGM-GNAZCLTHSA-N
  • Monoisotopic Mass: 244.097855505
  • Average Mass: 244.718
DBSALT000307
Pilocarpine nitrate
ThumbNot applicableDBSALT001181
Categories
UNII01MI4Q9DI3
CAS number92-13-7
WeightAverage: 208.2569
Monoisotopic: 208.121177766
Chemical FormulaC11H16N2O2
InChI KeyInChIKey=QCHFTSOMWOSFHM-WPRPVWTQSA-N
InChI
InChI=1S/C11H16N2O2/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2/h5,7-8,10H,3-4,6H2,1-2H3/t8-,10-/m0/s1
IUPAC Name
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]oxolan-2-one
SMILES
CC[[email protected]]1[C@@H](CC2=CN=CN2C)COC1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alkaloids and derivatives. These are naturally occurring chemical compounds that contain mostly basic nitrogen atoms. This group also includes some related compounds with neutral and even weakly acidic properties. Also some synthetic compounds of similar structure are attributed to alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and more rarely other elements such as chlorine, bromine, and phosphorus.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassNot Available
Sub ClassNot Available
Direct ParentAlkaloids and derivatives
Alternative Parents
Substituents
  • Pilocarpine
  • Alkaloid or derivatives
  • N-substituted imidazole
  • Gamma butyrolactone
  • Heteroaromatic compound
  • Oxolane
  • Imidazole
  • Azole
  • Lactone
  • Carboxylic acid ester
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome.
PharmacodynamicsPilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine.
Mechanism of actionPilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.
Related Articles
AbsorptionThere was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Possibly occurs at the neuronal synapses and in the plasma

Route of eliminationNot Available
Half life0.76 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+0.9816
Blood Brain Barrier+0.9758
Caco-2 permeable+0.6202
P-glycoprotein substrateNon-substrate0.5806
P-glycoprotein inhibitor INon-inhibitor0.8457
P-glycoprotein inhibitor IINon-inhibitor0.9432
Renal organic cation transporterNon-inhibitor0.6467
CYP450 2C9 substrateNon-substrate0.8408
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6665
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.8732
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.7961
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.6957
CarcinogenicityNon-carcinogens0.9166
BiodegradationNot ready biodegradable0.6808
Rat acute toxicity2.6826 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9432
hERG inhibition (predictor II)Non-inhibitor0.9009
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Suspensionophthalmic
Solutionophthalmic1 %
Liquidophthalmic2 %
Liquidophthalmic4 %
Dropsophthalmic
Solution/ dropsophthalmic10 mg/mL
Solution/ dropsophthalmic20 mg/mL
Solution/ dropsophthalmic40 mg/mL
Liquidophthalmic0.5 %
Liquidophthalmic10 mg
Liquidophthalmic20 mg
Liquidophthalmic40 mg
Liquidophthalmic60 g
Dropsophthalmic2 %
Dropsophthalmic4 %
Dropsophthalmic1 %
Dropsophthalmic6 %
Implantintraocular5 mg
Implantintraocular11 mg
Solutionophthalmic2 %
Solutionophthalmic4 %
Solutionophthalmic6 %
Solutionophthalmic10 mg/mL
Solutionophthalmic20 mg/mL
Solutionophthalmic40 mg/mL
Solutionophthalmic40 mg/1
Solution/ dropsconjunctival10 mg/mL
Tabletoral5 mg/1
Tablet, film coatedoral5 mg/1
Tablet, film coatedoral7.5 mg/1
Gelophthalmic4 %
Liquidophthalmic5 mg
Liquidophthalmic60 mg
Liquidophthalmic1 %
Tabletoral5 mg
Solutionophthalmic
Prices
Unit descriptionCostUnit
Pilopine HS 4% Gel 4 gm Tube64.08USD tube
Isopto Carpine 4% Solution 15ml Bottle37.5USD bottle
Isopto Carpine 4% Solution 30ml Bottle36.99USD bottle
Isopto Carpine 1% Solution 15ml Bottle36.37USD bottle
Isopto Carpine 2% Solution 15ml Bottle36.36USD bottle
Pilocarpine HCl 2% Solution 15ml Bottle35.01USD bottle
Isopto Carpine 2% Solution 30ml Bottle34.99USD bottle
Pilocarpine HCl 1% Solution 15ml Bottle32.24USD bottle
Pilocar 6% Solution 15ml Bottle15.99USD bottle
Pilopine hs 4% eye gel15.24USD g
Pilocar 4% Solution 15ml Bottle14.99USD bottle
Pilocar 1% Solution 15ml Bottle13.99USD bottle
Pilocar 2% Solution 15ml Bottle13.99USD bottle
Pilocar 0.5% Solution 15ml Bottle12.99USD bottle
Pilocarpine nitrate crystal9.85USD g
Pilocarpine hcl crystals8.19USD g
Pilocarpine 1% eye drops2.88USD ml
Pilocarpine 2% eye drops2.88USD ml
Pilocarpine 4% eye drops2.88USD ml
Pilopine Hs 4 % Gel2.81USD g
Salagen 7.5 mg tablet2.48USD tablet
Isopto carpine 4% eye drops2.37USD ml
Isopto carpine 2% eye drops2.26USD ml
Isopto carpine 1% eye drops2.21USD ml
Salagen 5 mg tablet2.14USD tablet
Pilocarpine hcl 7.5 mg tablet1.99USD tablet
Pilocarpine hcl 5 mg tablet1.55USD tablet
Salagen 5 mg Tablet1.23USD tablet
Pilocarpine 6% eye drops0.87USD ml
Piloptic-6 eye drops0.87USD ml
Piloptic-3 eye drops0.71USD ml
Pilocarpine 3% eye drops0.53USD ml
Pilocarpine 0.5% eye drops0.43USD ml
Isopto Carpine 4 % Solution0.3USD ml
Isopto Carpine 2 % Solution0.27USD ml
Isopto Carpine 1 % Solution0.23USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point204-205 °CPhysProp
water solubility1E+006 mg/L (at 25 °C)SEIDELL,A (1941)
logP1.1Not Available
pKa6.78Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.07 mg/mLALOGPS
logP1.15ALOGPS
logP0.95ChemAxon
logS-2ALOGPS
pKa (Strongest Basic)6.61ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area44.12 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity56.53 m3·mol-1ChemAxon
Polarizability22.34 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

Gerhard R. Reuther, “Process for the preparation of pilocarpine from in vitro cultures of pilocarpus.” U.S. Patent US5059531, issued June, 1987.

US5059531
General ReferencesNot Available
External Links
ATC CodesS01EB51S01EB01N07AX01
AHFS Codes
  • 12:04.00
  • 52:20.00
  • 92:02.00*
PDB EntriesNot Available
FDA labelDownload (160 KB)
MSDSDownload (73.3 KB)
Interactions
Drug Interactions
Drug
CimetropiumPilocarpine may decrease the anticholinergic activities of Cimetropium Bromide.
NadololThe risk or severity of adverse effects can be increased when Nadolol is combined with Pilocarpine.
TacrineThe risk or severity of adverse effects can be increased when Tacrine is combined with Pilocarpine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Sykes DA, Dowling MR, Charlton SJ: Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor. Mol Pharmacol. 2009 Sep;76(3):543-51. doi: 10.1124/mol.108.054452. Epub 2009 Jun 4. [PubMed:19498041 ]
  2. Figueroa KW, Griffin MT, Ehlert FJ: Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes. J Pharmacol Exp Ther. 2009 Jan;328(1):331-42. doi: 10.1124/jpet.108.145219. Epub 2008 Sep 29. [PubMed:18824613 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Figueroa KW, Griffin MT, Ehlert FJ: Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes. J Pharmacol Exp Ther. 2009 Jan;328(1):331-42. doi: 10.1124/jpet.108.145219. Epub 2008 Sep 29. [PubMed:18824613 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Moreno-Vinasco L, Verbout NG, Fryer AD, Jacoby DB: Retinoic acid prevents virus-induced airway hyperreactivity and M2 receptor dysfunction via anti-inflammatory and antiviral effects. Am J Physiol Lung Cell Mol Physiol. 2009 Aug;297(2):L340-6. doi: 10.1152/ajplung.90267.2008. Epub 2009 May 22. [PubMed:19465517 ]
  3. Figueroa KW, Griffin MT, Ehlert FJ: Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes. J Pharmacol Exp Ther. 2009 Jan;328(1):331-42. doi: 10.1124/jpet.108.145219. Epub 2008 Sep 29. [PubMed:18824613 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 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:
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23