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Identification
NamePancuronium
Accession NumberDB01337
TypeSmall Molecule
GroupsApproved
DescriptionA bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than curare but has less effect on the circulatory system and on histamine release.
Structure
Thumb
Synonyms
Bromure de pancuronium
Bromuro de pancuronio
Pancuronium
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pancuronium Bromide - Liq IV 1mg/mlliquid1 mgintravenousSandoz Canada Incorporated1995-12-31Not applicableCanada
Pancuronium Bromide - Liq IV 2mg/mlliquid2 mgintravenousSandoz Canada Incorporated1996-12-31Not applicableCanada
Pancuronium Bromide 1mg/mlsolution1 mgintravenousHospira Healthcare Corporation1996-10-24Not applicableCanada
Pancuronium Bromide 2mg/mlsolution2 mgintravenousHospira Healthcare Corporation1995-12-31Not applicableCanada
Pavulon Inj 1mg/mlliquid1 mgintravenousOrganon Canada Ltd Ltee1979-12-311997-08-18Canada
Pavulon Inj 2mg/mlliquid2 mgintravenousOrganon Canada Ltd Ltee1973-12-311997-08-18Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pancuronium Bromideinjection, solution1 mg/mLintravenousHospira, Inc.1989-01-19Not applicableUs
Pancuronium Bromideinjection, solution1 mg/mLintravenousTeva Parenteral Medicines, Inc.1990-08-01Not applicableUs
Pancuronium Bromideinjection, solution2 mg/mLintravenousTeva Parenteral Medicines, Inc.1990-08-01Not applicableUs
Pancuronium Bromideinjection, solution2 mg/mLintravenousTeva Parenteral Medicines, Inc.1990-08-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MioblockNot Available
PavulonNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Pancuronium bromide
15500-66-0
Thumb
  • InChI Key: NPIJXCQZLFKBMV-YTGGZNJNSA-L
  • Monoisotopic Mass: 730.291983712
  • Average Mass: 732.67
DBSALT000368
Categories
UNIIJ76UF062FS
CAS numberNot Available
WeightAverage: 572.8619
Monoisotopic: 572.455308418
Chemical FormulaC35H60N2O4
InChI KeyInChIKey=GVEAYVLWDAFXET-XGHATYIMSA-N
InChI
InChI=1S/C35H60N2O4/c1-24(38)40-32-21-26-13-14-27-28(35(26,4)23-31(32)37(6)19-11-8-12-20-37)15-16-34(3)29(27)22-30(33(34)41-25(2)39)36(5)17-9-7-10-18-36/h26-33H,7-23H2,1-6H3/q+2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-/m0/s1
IUPAC Name
1-[(1S,2S,4S,5S,7S,10R,11S,13S,14R,15S)-5,14-bis(acetyloxy)-2,15-dimethyl-13-(1-methylpiperidin-1-ium-1-yl)tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-4-yl]-1-methylpiperidin-1-ium
SMILES
[H][C@@]12C[C@@H]([[email protected]](OC(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])C[[email protected]](OC(C)=O)[[email protected]](C[C@]12C)[N+]1(C)CCCCC1)[N+]1(C)CCCCC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassSteroid esters
Direct ParentSteroid esters
Alternative Parents
Substituents
  • Steroid ester
  • Androstane-skeleton
  • Cyclohexylamine
  • Piperidine
  • Acetate salt
  • Quaternary ammonium salt
  • Carboxylic acid ester
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Organic cation
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed as a muscle relaxant during anesthesia and surgical procedures.
PharmacodynamicsPancuronium is a typical non-depolarising curare-mimetic muscle relaxant. It acts as a competitive acetylcholine antagonist on neuromuscular junctions, displacing acetylcholine (hence competitive) from its post-synaptic nicotinic acetylcholine receptors. It is, unlike suxamethonium, a non-depolarising agent, which means, that it causes no spontaneous depolarisations upon association with the nicotinic receptor in neuromuscular junction, thus producing no muscle fasciculations upon administration. Pancuronium has no hormonal activity. It exerts slight vagolytic activity (i.e. diminishing activity of the vagus nerve) and no ganglioplegic (i.e., blocking ganglions) activity.
Mechanism of actionNondepolarizing neuromuscular blocking agents inhibit neuromuscular transmission by competing with acetylcholine for the cholinergic receptors of the motor end plate, thereby reducing the response of the end plate to acetylcholine. This type of neuromuscular block is usually antagonized by anticholinesterase agents.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 241 to 280 mL/kg
Protein binding77 to 91%
Metabolism

Hepatic.

Route of eliminationNot Available
Half life1.5 to 2.7 hours.
Clearance
  • Plasma cl=1.1–1.9 mL/minute/kg
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-0.8913
Blood Brain Barrier+0.878
Caco-2 permeable+0.5457
P-glycoprotein substrateSubstrate0.77
P-glycoprotein inhibitor IInhibitor0.6962
P-glycoprotein inhibitor IIInhibitor0.6508
Renal organic cation transporterNon-inhibitor0.6862
CYP450 2C9 substrateNon-substrate0.8382
CYP450 2D6 substrateNon-substrate0.7638
CYP450 3A4 substrateSubstrate0.742
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9229
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9368
Ames testNon AMES toxic0.7499
CarcinogenicityNon-carcinogens0.9265
BiodegradationNot ready biodegradable0.8557
Rat acute toxicity2.6653 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9021
hERG inhibition (predictor II)Non-inhibitor0.7784
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous1 mg/mL
Injection, solutionintravenous2 mg/mL
Liquidintravenous1 mg
Liquidintravenous2 mg
Solutionintravenous1 mg
Solutionintravenous2 mg
Prices
Unit descriptionCostUnit
Pancuronium 2 mg/ml vial2.59USD ml
Pancuronium 1 mg/ml vial0.13USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point215 °CPhysProp
water solubility5E+005 mg/LMERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility3.08e-06 mg/mLALOGPS
logP1.04ALOGPS
logP-3.3ChemAxon
logS-8.3ALOGPS
pKa (Strongest Basic)-6.7ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area52.6 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity185.22 m3·mol-1ChemAxon
Polarizability69.44 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesM03AC01
AHFS Codes
  • 12:20.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with 1,10-Phenanthroline.
AclidiniumAclidinium may increase the anticholinergic activities of Pancuronium.
AclidiniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Aclidinium.
AlfentanilThe risk or severity of adverse effects can be increased when Pancuronium is combined with Alfentanil.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Pancuronium is combined with Alphacetylmethadol.
AmbenoniumThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Ambenonium.
AminophyllineThe risk or severity of adverse effects can be increased when Aminophylline is combined with Pancuronium.
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Pancuronium.
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Pancuronium.
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Pancuronium.
BenactyzineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Benactyzine.
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Pancuronium.
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Pancuronium.
BezitramideThe risk or severity of adverse effects can be increased when Pancuronium is combined with Bezitramide.
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Pancuronium.
Botulinum Toxin Type APancuronium may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BPancuronium may increase the anticholinergic activities of Botulinum Toxin Type B.
BuprenorphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Buprenorphine.
ButorphanolThe risk or severity of adverse effects can be increased when Pancuronium is combined with Butorphanol.
CarfentanilThe risk or severity of adverse effects can be increased when Pancuronium is combined with Carfentanil.
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Pancuronium.
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Chlorphenoxamine.
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Pancuronium.
CimetropiumPancuronium may increase the anticholinergic activities of Cimetropium.
CodeineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Codeine.
CoumaphosThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Coumaphos.
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Pancuronium.
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pancuronium.
DecamethoniumThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Decamethonium.
DemecariumThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Demecarium.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Pancuronium.
DexetimideThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dexetimide.
DextromoramideThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dextromoramide.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dextropropoxyphene.
DezocineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dezocine.
DichlorvosThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Dichlorvos.
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Pancuronium.
DihydrocodeineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dihydrocodeine.
DihydroetorphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dihydroetorphine.
DihydromorphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Dihydromorphine.
DiphenoxylateThe risk or severity of adverse effects can be increased when Pancuronium is combined with Diphenoxylate.
DonepezilThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Donepezil.
DPDPEThe risk or severity of adverse effects can be increased when Pancuronium is combined with DPDPE.
DronabinolPancuronium may increase the tachycardic activities of Dronabinol.
DyphyllineThe risk or severity of adverse effects can be increased when Dyphylline is combined with Pancuronium.
EchothiophateThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Echothiophate.
EdrophoniumThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Edrophonium.
EluxadolinePancuronium may increase the constipating activities of Eluxadoline.
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Pancuronium.
EthylmorphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Ethylmorphine.
EtorphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Etorphine.
FentanylThe risk or severity of adverse effects can be increased when Pancuronium is combined with Fentanyl.
FenthionThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Fenthion.
FesoterodineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Fesoterodine.
GalantamineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Galantamine.
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pancuronium.
Ginkgo bilobaThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Ginkgo biloba.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Pancuronium is combined with Glucagon recombinant.
GlycopyrroniumThe risk or severity of adverse effects can be increased when Glycopyrronium is combined with Pancuronium.
GlycopyrroniumPancuronium may increase the anticholinergic activities of Glycopyrronium.
HeroinThe risk or severity of adverse effects can be increased when Pancuronium is combined with Heroin.
HexamethoniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Hexamethonium.
HomatropineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Homatropine.
Huperzine AThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Huperzine A.
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Pancuronium.
HydrocodoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Hydrocodone.
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Pancuronium.
HydromorphoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Hydromorphone.
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Pancuronium.
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Pancuronium.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Pancuronium.
IsoflurophateThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Isoflurophate.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Pancuronium.
KetobemidoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Ketobemidone.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Pancuronium is combined with Levomethadyl Acetate.
LevorphanolThe risk or severity of adverse effects can be increased when Pancuronium is combined with Levorphanol.
LofentanilThe risk or severity of adverse effects can be increased when Pancuronium is combined with Lofentanil.
MalathionThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Malathion.
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Pancuronium.
MefloquineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Mefloquine.
MemantineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Memantine.
MethadoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Methadone.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Pancuronium is combined with Methadyl Acetate.
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Pancuronium.
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Pancuronium.
MetixeneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Metixene.
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Pancuronium.
MianserinMianserin may increase the anticholinergic activities of Pancuronium.
MinaprineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Minaprine.
MirabegronThe risk or severity of adverse effects can be increased when Pancuronium is combined with Mirabegron.
MorphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Morphine.
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when Pancuronium is combined with N-butylscopolammonium bromide.
NabilonePancuronium may increase the tachycardic activities of Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Nalbuphine.
NeostigmineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Neostigmine.
NormethadoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Normethadone.
NVA237The risk or severity of adverse effects can be increased when Pancuronium is combined with NVA237.
OpiumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Opium.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Pancuronium.
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Pancuronium.
OxycodoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Oxycodone.
OxymorphoneThe risk or severity of adverse effects can be increased when Pancuronium is combined with Oxymorphone.
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Pancuronium.
PentazocineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Pentazocine.
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Pancuronium.
PethidineThe risk or severity of adverse effects can be increased when Pancuronium is combined with Pethidine.
PhysostigmineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Physostigmine.
PipecuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Pipecuronium.
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Pancuronium.
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Pancuronium.
Potassium ChloridePancuronium may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Pancuronium.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Pancuronium.
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Pancuronium.
PyridostigmineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Pyridostigmine.
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Pancuronium.
QuinidineThe risk or severity of adverse effects can be increased when Quinidine is combined with Pancuronium.
RamosetronPancuronium may increase the constipating activities of Ramosetron.
RemifentanilThe risk or severity of adverse effects can be increased when Pancuronium is combined with Remifentanil.
RivastigmineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Rivastigmine.
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Pancuronium.
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Pancuronium is combined with Scopolamine butylbromide.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Pancuronium.
SolifenacinThe risk or severity of adverse effects can be increased when Pancuronium is combined with Solifenacin.
SufentanilThe risk or severity of adverse effects can be increased when Pancuronium is combined with Sufentanil.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Pancuronium.
TacrineThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Tacrine.
TapentadolThe risk or severity of adverse effects can be increased when Pancuronium is combined with Tapentadol.
TheophyllineThe risk or severity of adverse effects can be increased when Theophylline is combined with Pancuronium.
TiotropiumPancuronium may increase the anticholinergic activities of Tiotropium.
TiotropiumThe risk or severity of adverse effects can be increased when Tiotropium is combined with Pancuronium.
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pancuronium.
TopiramateThe risk or severity of adverse effects can be increased when Pancuronium is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Pancuronium is combined with Tramadol.
TrichlorfonThe therapeutic efficacy of Pancuronium can be decreased when used in combination with Trichlorfon.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Pancuronium.
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pancuronium.
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Pancuronium.
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pancuronium.
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Pancuronium.
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Pancuronium.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Pancuronium.
UmeclidiniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Umeclidinium.
VecuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Vecuronium.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Drug binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name:
CHRNA2
Uniprot ID:
Q15822
Molecular Weight:
59764.82 Da
References
  1. 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 ]
  2. Dilger JP, Vidal AM, Liu M, Mettewie C, Suzuki T, Pham A, Demazumder D: Roles of amino acids and subunits in determining the inhibition of nicotinic acetylcholine receptors by competitive antagonists. Anesthesiology. 2007 Jun;106(6):1186-95. [PubMed:17525594 ]
  3. Jonsson Fagerlund M, Dabrowski M, Eriksson LI: Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52. doi: 10.1097/ALN.0b013e31819fade3. [PubMed:19417616 ]
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. Milchert M, Spassov A, Meissner K, Nedeljkov V, Lehmann C, Wendt M, Loster BW, Mazurkiewicz-Janik M, Gedrange T, Pavlovic D: Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro. J Physiol Pharmacol. 2009 Dec;60 Suppl 8:5-11. [PubMed:20400785 ]
  2. Cembala TM, Forde SC, Appadu BL, Lambert DG: Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors. Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22. [PubMed:17588565 ]
  3. Okanlami OA, Fryer AD, Hirshman C: Interaction of nondepolarizing muscle relaxants with M2 and M3 muscarinic receptors in guinea pig lung and heart. Anesthesiology. 1996 Jan;84(1):155-61. [PubMed:8572329 ]
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. Milchert M, Spassov A, Meissner K, Nedeljkov V, Lehmann C, Wendt M, Loster BW, Mazurkiewicz-Janik M, Gedrange T, Pavlovic D: Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro. J Physiol Pharmacol. 2009 Dec;60 Suppl 8:5-11. [PubMed:20400785 ]
  2. Okanlami OA, Fryer AD, Hirshman C: Interaction of nondepolarizing muscle relaxants with M2 and M3 muscarinic receptors in guinea pig lung and heart. Anesthesiology. 1996 Jan;84(1):155-61. [PubMed:8572329 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Identical protein binding
Specific Function:
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name:
BCHE
Uniprot ID:
P06276
Molecular Weight:
68417.575 Da
References
  1. Stovner J, Oftedal N, Holmboe J: The inhibition of cholinesterases by pancuronium. Br J Anaesth. 1975 Sep;47(9):949-54. [PubMed:1191483 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM: Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997 Jun;51(6):913-21. [PubMed:9187257 ]
  2. Busch AE, Quester S, Ulzheimer JC, Waldegger S, Gorboulev V, Arndt P, Lang F, Koepsell H: Electrogenic properties and substrate specificity of the polyspecific rat cation transporter rOCT1. J Biol Chem. 1996 Dec 20;271(51):32599-604. [PubMed:8955087 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H: Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81. [PubMed:9260930 ]
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Drug created on June 30, 2007 12:07 / Updated on August 17, 2016 12:23