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Identification
NameMetixene
Accession NumberDB00340  (APRD01101)
TypeSmall Molecule
GroupsApproved
DescriptionMetixene (or methixene) is a anticholinergic used as an antiparkinsonian agent.
Structure
Thumb
Synonyms
Methixen
Methixene
Metisene
Metixeno
Metixenum
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CholinfallNot Available
MethixartNot Available
TremarilNot Available
TremaritNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Metixene hydrochloride
Thumb
  • InChI Key: RSXZRFHNNTTWCB-UHFFFAOYNA-N
  • Monoisotopic Mass: 345.13179817
  • Average Mass: 345.929
DBSALT000602
Categories
UNII32VY6L26ZW
CAS number4969-02-2
WeightAverage: 309.468
Monoisotopic: 309.155120431
Chemical FormulaC20H23NS
InChI KeyMJFJKKXQDNNUJF-UHFFFAOYSA-N
InChI
InChI=1S/C20H23NS/c1-21-12-6-7-15(14-21)13-18-16-8-2-4-10-19(16)22-20-11-5-3-9-17(18)20/h2-5,8-11,15,18H,6-7,12-14H2,1H3
IUPAC Name
1-methyl-3-(9H-thioxanthen-9-ylmethyl)piperidine
SMILES
CN1CCCC(CC2C3=CC=CC=C3SC3=CC=CC=C23)C1
Pharmacology
IndicationUsed for the symptomatic treatment of parkinsonism.
Structured Indications Not Available
PharmacodynamicsMetixene is a tertiary antimuscarinic with actions similar to those of atropine; it also has antihistaminic and direct antispasmodic properties. It is used for the symptomatic treatment of parkinsonism, including the alleviation of the extrapyramidal syndrome induced by other drugs such as phenothiazines, but, like other antimuscarinics, it is of no value against tardive dyskinesias. Metixene has been discontinued.
Mechanism of actionParkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as metixene is considered to relate to competitive antagonism of acetylcholine at muscarinic receptors in the corpus striatum, which then restores the balance.
TargetKindPharmacological actionActionsOrganismUniProt ID
Muscarinic acetylcholine receptor M1Proteinyes
antagonist
HumanP11229 details
Muscarinic acetylcholine receptor M4Proteinyes
antagonist
HumanP08173 details
Muscarinic acetylcholine receptor M5Proteinyes
antagonist
HumanP08912 details
Muscarinic acetylcholine receptor M2Proteinunknown
antagonist
HumanP08172 details
Muscarinic acetylcholine receptor M3Proteinunknown
antagonist
HumanP20309 details
Related Articles
AbsorptionAbsorbed in the gastrointestinal tract following oral administration, however the extent of absorption is not known.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic. Metabolism occurs via sulfoxydation and N-demethylation.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySigns of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Metixene can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AclidiniumAclidinium may increase the anticholinergic activities of Metixene.Approved
AlfentanilThe risk or severity of adverse effects can be increased when Metixene is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Metixene is combined with Alphacetylmethadol.Experimental, Illicit
AmbenoniumThe therapeutic efficacy of Metixene can be decreased when used in combination with Ambenonium.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Metixene.Approved
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Metixene.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Metixene.Approved, Vet Approved
BenactyzineThe risk or severity of adverse effects can be increased when Benactyzine is combined with Metixene.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Metixene.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Metixene.Approved
BezitramideThe risk or severity of adverse effects can be increased when Metixene is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Metixene.Approved
Botulinum Toxin Type AMetixene may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BMetixene may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Metixene is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Metixene is combined with Butorphanol.Approved, Illicit, Vet Approved
CarfentanilThe risk or severity of adverse effects can be increased when Metixene is combined with Carfentanil.Illicit, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Metixene.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Chlorphenoxamine is combined with Metixene.Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Metixene.Approved
CimetropiumMetixene may increase the anticholinergic activities of Cimetropium.Experimental
CodeineThe risk or severity of adverse effects can be increased when Metixene is combined with Codeine.Approved, Illicit
CoumaphosThe therapeutic efficacy of Metixene can be decreased when used in combination with Coumaphos.Vet Approved
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Metixene.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Metixene.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Metixene can be decreased when used in combination with Decamethonium.Approved
DemecariumThe therapeutic efficacy of Metixene can be decreased when used in combination with Demecarium.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Metixene.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Metixene.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Metixene is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Metixene is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Metixene is combined with Dezocine.Approved
DichlorvosThe therapeutic efficacy of Metixene can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Metixene.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Metixene is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Metixene is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Metixene is combined with Dihydromorphine.Experimental, Illicit
DiphenoxylateThe risk or severity of adverse effects can be increased when Metixene is combined with Diphenoxylate.Approved, Illicit
DonepezilThe therapeutic efficacy of Metixene can be decreased when used in combination with Donepezil.Approved
DPDPEThe risk or severity of adverse effects can be increased when Metixene is combined with DPDPE.Investigational
DronabinolMetixene may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Metixene can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Metixene can be decreased when used in combination with Edrophonium.Approved
EluxadolineMetixene may increase the constipating activities of Eluxadoline.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Metixene.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Metixene is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Metixene is combined with Etorphine.Illicit, Vet Approved
FentanylThe risk or severity of adverse effects can be increased when Metixene is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Metixene can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Metixene.Approved
GalantamineThe therapeutic efficacy of Metixene can be decreased when used in combination with Galantamine.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Metixene.Approved
Ginkgo bilobaThe therapeutic efficacy of Metixene can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Metixene is combined with Glucagon recombinant.Approved
GlycopyrroniumMetixene may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Metixene is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Hexamethonium is combined with Metixene.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Metixene is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Metixene can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Metixene.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Metixene is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Metixene.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Metixene is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Metixene.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Metixene.Approved
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Metixene.Approved
IsoflurophateThe therapeutic efficacy of Metixene can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Metixene.Investigational
KetobemidoneThe risk or severity of adverse effects can be increased when Metixene is combined with Ketobemidone.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Metixene is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Metixene is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Metixene is combined with Lofentanil.Illicit
MalathionThe therapeutic efficacy of Metixene can be decreased when used in combination with Malathion.Approved, Investigational
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Metixene.Approved
MefloquineThe therapeutic efficacy of Metixene can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Metixene can be decreased when used in combination with Memantine.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Metixene is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Metixene is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Metixene can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Metixene.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Metixene.Approved
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Metixene.Approved
MianserinMianserin may increase the anticholinergic activities of Metixene.Approved
MinaprineThe therapeutic efficacy of Metixene can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Metixene is combined with Mirabegron.Approved
MorphineThe risk or severity of adverse effects can be increased when Metixene is combined with Morphine.Approved, Investigational
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when N-butylscopolammonium bromide is combined with Metixene.Vet Approved
NabiloneMetixene may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Metixene is combined with Nalbuphine.Approved
NeostigmineThe therapeutic efficacy of Metixene can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Metixene is combined with Normethadone.Approved, Illicit
NVA237The risk or severity of adverse effects can be increased when NVA237 is combined with Metixene.Investigational
OpiumThe risk or severity of adverse effects can be increased when Metixene is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Metixene.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Metixene.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Metixene is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Metixene is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Metixene.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Metixene.Approved
PentazocineThe risk or severity of adverse effects can be increased when Metixene is combined with Pentazocine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Metixene.Approved
PethidineThe risk or severity of adverse effects can be increased when Metixene is combined with Pethidine.Approved
PhysostigmineThe therapeutic efficacy of Metixene can be decreased when used in combination with Physostigmine.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Pipecuronium is combined with Metixene.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Metixene.Approved
PiritramideThe risk or severity of adverse effects can be increased when Metixene is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Metixene.Approved
Potassium ChlorideMetixene may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Metixene.Approved, Investigational
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Metixene.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Metixene.Approved
PropiverineThe risk or severity of adverse effects can be increased when Metixene is combined with Propiverine.Investigational
PyridostigmineThe therapeutic efficacy of Metixene can be decreased when used in combination with Pyridostigmine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Metixene.Approved
QuinidineThe risk or severity of adverse effects can be increased when Quinidine is combined with Metixene.Approved
RamosetronMetixene may increase the constipating activities of Ramosetron.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Metixene is combined with Remifentanil.Approved
RivastigmineThe therapeutic efficacy of Metixene can be decreased when used in combination with Rivastigmine.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Metixene.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Scopolamine butylbromide is combined with Metixene.Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Metixene.Approved, Investigational
SolifenacinThe risk or severity of adverse effects can be increased when Solifenacin is combined with Metixene.Approved
SufentanilThe risk or severity of adverse effects can be increased when Metixene is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Metixene.Approved
TacrineThe therapeutic efficacy of Metixene can be decreased when used in combination with Tacrine.Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Metixene is combined with Tapentadol.Approved
TiotropiumMetixene may increase the anticholinergic activities of Tiotropium.Approved
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Metixene.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Metixene is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Metixene is combined with Tramadol.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Metixene can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Metixene.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Metixene.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Metixene.Approved
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Metixene.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Metixene.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Metixene.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Metixene.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Metixene.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Link [Link]
External Links
ATC CodesN04AA03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9825
Blood Brain Barrier+0.995
Caco-2 permeable+0.7863
P-glycoprotein substrateSubstrate0.81
P-glycoprotein inhibitor IInhibitor0.51
P-glycoprotein inhibitor IIInhibitor0.8379
Renal organic cation transporterInhibitor0.8034
CYP450 2C9 substrateNon-substrate0.7575
CYP450 2D6 substrateSubstrate0.7452
CYP450 3A4 substrateNon-substrate0.5709
CYP450 1A2 substrateNon-inhibitor0.8941
CYP450 2C9 inhibitorNon-inhibitor0.9516
CYP450 2D6 inhibitorInhibitor0.9146
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.951
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6914
Ames testNon AMES toxic0.8216
CarcinogenicityNon-carcinogens0.9644
BiodegradationNot ready biodegradable0.973
Rat acute toxicity2.4059 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6823
hERG inhibition (predictor II)Inhibitor0.8044
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point< 25 °CPhysProp
boiling point173 °C at 7.00E-02 mm HgPhysProp
water solubilitySoluble as HCl saltNot Available
logP4.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000102 mg/mLALOGPS
logP5.51ALOGPS
logP5.06ChemAxon
logS-6.5ALOGPS
pKa (Strongest Basic)9.34ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity97.17 m3·mol-1ChemAxon
Polarizability35.67 Å3ChemAxon
Number of Rings4ChemAxon
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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as thioxanthenes. These are organic polycyclic compounds containing a thioxanthene moiety, which is an aromatic tricycle derived from xanthene by replacing the oxygen atom with a sulfur atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiopyrans
Sub Class1-benzothiopyrans
Direct ParentThioxanthenes
Alternative Parents
Substituents
  • Thioxanthene
  • Diarylthioether
  • Aralkylamine
  • Benzenoid
  • Piperidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
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 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor 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 inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 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 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
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:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 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. 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:
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. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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. 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23