Cisatracurium besylate

Identification

Name
Cisatracurium besylate
Accession Number
DB00565  (APRD00874)
Type
Small Molecule
Groups
Approved
Description

Cisatracurium is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.

Structure
Thumb
Synonyms
  • (1R-cis,1'R-cis)-2,2'-{pentane-1,5-diylbis[oxy(3-oxopropane-3,1-diyl)]}bis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolinium] bisbenzenesulfonate
  • (1R-cis,1'R-cis)-atracurium besylate
  • (1R,1'R,2R,2'r)-atracurium besylate
  • Besilate de cisatracurium
  • Besilato de cisatracurio
  • Cisatracurii besilas
  • Cisatracurium besilate
  • Cisatracurium dibenzenesulfonate
  • Cisatracurium-Kation
External IDs
51-W89 / 51W-89 / 51W89
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cisatracurium Besylate InjectionSolution2 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Cisatracurium Besylate InjectionSolution2 mgIntravenousAccord Healthcare LimitedNot applicableNot applicableCanada
Cisatracurium Besylate Injection (preservative-free)Solution2 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Cisatracurium Besylate Injection Multi-doseSolution2 mgIntravenousFresenius KabiNot applicableNot applicableCanada
Cisatracurium Besylate Injection Single DoseSolution2 mgIntravenousFresenius KabiNot applicableNot applicableCanada
Cisatracurium Omega MultidoseSolution2 mgIntravenousOmega Laboratories Ltd2014-01-20Not applicableCanada
NimbexInjection2 mg/mLIntravenousAbbvie2010-12-09Not applicableUs
NimbexInjection10 mg/mLIntravenousAbbvie1995-12-15Not applicableUs
NimbexLiquid2 mgIntravenousAbbvie1997-04-072016-06-07Canada
NimbexInjection2 mg/mLIntravenousAbbvie2010-12-09Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aj-cisatracuriumSolution2 mgIntravenousAgila Jamp Canada IncNot applicableNot applicableCanada
Aj-cisatracuriumSolution2 mgIntravenousAgila Jamp Canada IncNot applicableNot applicableCanada
CisatracuriumInjection, solution2 mg/mLIntravenousFresenius Kabi2015-02-26Not applicableUs
CisatracuriumInjection, solution10 mg/mLIntravenousFresenius Kabi2015-02-26Not applicableUs
CisatracuriumInjection, solution2 mg/mLIntravenousFresenius Kabi2015-02-26Not applicableUs
Cisatracurium BesylateInjection, solution2 mg/mLIntravenousSagent Pharmaceuticals2012-09-272016-10-21Us
Cisatracurium BesylateInjection2 mg/mLIntravenousJiangsu Hengrui Medicine Co., Ltd.2017-08-31Not applicableUs
Cisatracurium BesylateInjection10 mg/mLIntravenousSandoz2012-07-16Not applicableUs
Cisatracurium BesylateInjection2 mg/mLIntravenousSandoz2013-02-28Not applicableUs
Cisatracurium BesylateInjection, solution2 mg/mLIntravenousSagent Pharmaceuticals2012-09-272016-10-21Us
International/Other Brands
Nimbex Forte (GlaxoSmithKline) / Nimbium (GlaxoSmithKline)
Categories
UNII
80YS8O1MBS
CAS number
96946-42-8
Weight
Average: 1243.479
Monoisotopic: 1242.50040521
Chemical Formula
C65H82N2O18S2
InChI Key
XXZSQOVSEBAPGS-DONVQRBFSA-L
InChI
InChI=1S/C53H72N2O12.2C6H6O3S/c1-54(22-18-38-32-48(62-7)50(64-9)34-40(38)42(54)28-36-14-16-44(58-3)46(30-36)60-5)24-20-52(56)66-26-12-11-13-27-67-53(57)21-25-55(2)23-19-39-33-49(63-8)51(65-10)35-41(39)43(55)29-37-15-17-45(59-4)47(31-37)61-6;2*7-10(8,9)6-4-2-1-3-5-6/h14-17,30-35,42-43H,11-13,18-29H2,1-10H3;2*1-5H,(H,7,8,9)/q+2;;/p-2/t42-,43-,54-,55-;;/m1../s1
IUPAC Name
(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-2-(3-{[5-({3-[(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-2-ium-2-yl]propanoyl}oxy)pentyl]oxy}-3-oxopropyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-2-ium dibenzenesulfonate
SMILES
[O-]S(=O)(=O)C1=CC=CC=C1.[O-]S(=O)(=O)C1=CC=CC=C1.COC1=C(OC)C=C(C[[email protected]@H]2C3=CC(OC)=C(OC)C=C3CC[[email protected]+]2(C)CCC(=O)OCCCCCOC(=O)CC[[email protected]@+]2(C)CCC3=CC(OC)=C(OC)C=C3[[email protected]]2CC2=CC(OC)=C(OC)C=C2)C=C1

Pharmacology

Indication

For inpatients and outpatients as an adjunct to general anesthesia, to facilitate tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation in the ICU.

Structured Indications
Not Available
Pharmacodynamics

Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antagonized by anticholinesterase agents once recovery has started. As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.

Mechanism of action

Cisatracurium Besylate binds to the nicotinic acetycholine (cholinergic) receptors in the motor endplate and blocks access to the receptors. In the process of binding, the receptor is actually activated - causing a process known as depolarization. Since it is not degraded in the neuromuscular junction, the depolarized membrane remains depolarized and unresponsive to any other impulse, causing muscle paralysis.

TargetActionsOrganism
ANeuronal acetylcholine receptor subunit alpha-2
inhibitor
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

The binding of cisatracurium to plasma proteins has not been successfully studied due to its rapid degradation at physiologic pH.

Metabolism

The degradation of cisatracurium is largely independent of liver metabolism. Results from in vitro experiments suggest that cisatracurium undergoes Hofmann elimination (a pH and temperature-dependent chemical process) to form laudanosine and the monoquaternary acrylate metabolite. The monoquaternary acrylate undergoes hydrolysis by non-specific plasma esterases to form the monoquaternary alcohol metabolite. The monoquaternary alcohol metabolite can also undergo Hofmann elimination but at a much slower rate than cisatracurium. Laudanosine is further metabolized to desmethyl metabolites which are conjugated with glucuronic acid and excreted in the urine.

Route of elimination

Biliary and urinary excretion were the major routes of excretion of radioactivity (totaling >90% of the labeled dose within 7 hours of dosing), of which atracurium represented only a minor fraction.

Half life

Elimination half-life of 22 minutes.

Clearance
Not Available
Toxicity

Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.

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

Interactions

Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinCisatracurium besylate may increase the arrhythmogenic activities of Acetyldigitoxin.Approved
AcetyldigoxinCisatracurium besylate may increase the arrhythmogenic activities of Acetyldigoxin.Experimental
AclarubicinAclarubicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
AldoxorubicinAldoxorubicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
AmikacinAmikacin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Vet Approved
AmrubicinAmrubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
AnnamycinAnnamycin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
ApramycinApramycin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental, Vet Approved
ArbekacinArbekacin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
BekanamycinBekanamycin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
Botulinum Toxin Type ABotulinum Toxin Type A may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Investigational
Botulinum Toxin Type BCisatracurium besylate may increase the neuromuscular blocking activities of Botulinum Toxin Type B.Approved
BumetanideBumetanide may decrease the neuromuscular blocking activities of Cisatracurium besylate.Approved
CapreomycinCapreomycin may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
ChlortetracyclineChlortetracycline may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Investigational, Vet Approved
ClindamycinClindamycin may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Vet Approved
ColistimethateColistimethate may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Vet Approved
CyclosporineCyclosporine may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Investigational, Vet Approved
CymarinCisatracurium besylate may increase the arrhythmogenic activities of Cymarin.Experimental
DaunorubicinDaunorubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
DemeclocyclineDemeclocycline may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
DeslanosideCisatracurium besylate may increase the arrhythmogenic activities of Deslanoside.Approved
DibekacinDibekacin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
DigitoxinCisatracurium besylate may increase the arrhythmogenic activities of Digitoxin.Approved, Investigational
DigoxinCisatracurium besylate may increase the arrhythmogenic activities of Digoxin.Approved
Digoxin Immune Fab (Ovine)Cisatracurium besylate may increase the arrhythmogenic activities of Digoxin Immune Fab (Ovine).Approved
DihydrostreptomycinDihydrostreptomycin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational, Vet Approved
DoxorubicinDoxorubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
DoxycyclineDoxycycline may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Investigational, Vet Approved
EpirubicinEpirubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
Etacrynic acidEtacrynic acid may decrease the neuromuscular blocking activities of Cisatracurium besylate.Approved
FramycetinFramycetin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
FurosemideFurosemide may decrease the neuromuscular blocking activities of Cisatracurium besylate.Approved, Vet Approved
GeneticinGeneticin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
GentamicinGentamicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Vet Approved
GENTAMICIN C1AGENTAMICIN C1A may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
GitoformateCisatracurium besylate may increase the arrhythmogenic activities of Gitoformate.Experimental
GPX-150GPX-150 may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
Hygromycin BHygromycin B may increase the respiratory depressant activities of Cisatracurium besylate.Vet Approved
IdarubicinIdarubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
IsepamicinIsepamicin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
KanamycinKanamycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational, Vet Approved
Lanatoside CCisatracurium besylate may increase the arrhythmogenic activities of Lanatoside C.Experimental
LincomycinLincomycin may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Vet Approved
LithiumLithium may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
Magnesium HydroxideMagnesium Hydroxide may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
Magnesium oxideMagnesium oxide may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
Magnesium salicylateMagnesium salicylate may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
Magnesium SulfateMagnesium Sulfate may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Vet Approved
MetildigoxinCisatracurium besylate may increase the arrhythmogenic activities of Metildigoxin.Experimental
MetrizamideMetrizamide may increase the respiratory depressant activities of Cisatracurium besylate.Approved
MicronomicinMicronomicin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
MinocyclineMinocycline may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Investigational
NeamineNeamine may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
NeomycinNeomycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Vet Approved
NetilmicinNetilmicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
OleandrinCisatracurium besylate may increase the arrhythmogenic activities of Oleandrin.Experimental, Investigational
OuabainCisatracurium besylate may increase the arrhythmogenic activities of Ouabain.Approved
ParomomycinParomomycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
PeruvosideCisatracurium besylate may increase the arrhythmogenic activities of Peruvoside.Experimental
PirarubicinPirarubicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
PiretanidePiretanide may decrease the neuromuscular blocking activities of Cisatracurium besylate.Experimental
PirlimycinPirlimycin may increase the neuromuscular blocking activities of Cisatracurium besylate.Vet Approved
PlazomicinPlazomicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
PlicamycinPlicamycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational, Withdrawn
Polymyxin B SulfatePolymyxin B Sulfate may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved, Vet Approved
ProcainamideProcainamide may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
ProscillaridinCisatracurium besylate may increase the arrhythmogenic activities of Proscillaridin.Experimental
PuromycinPuromycin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
QuinidineQuinidine may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
QuinineQuinine may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
RibostamycinRibostamycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
SabarubicinSabarubicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
SisomicinSisomicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
SP1049CSP1049C may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
SpectinomycinSpectinomycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational, Vet Approved
StreptomycinStreptomycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Vet Approved
StreptozocinStreptozocin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
TobramycinTobramycin may increase the respiratory depressant activities of Cisatracurium besylate.Approved, Investigational
TorasemideTorasemide may decrease the neuromuscular blocking activities of Cisatracurium besylate.Approved
ValrubicinValrubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
VancomycinVancomycin may increase the neuromuscular blocking activities of Cisatracurium besylate.Approved
Zoptarelin doxorubicinZoptarelin doxorubicin may increase the respiratory depressant activities of Cisatracurium besylate.Investigational
ZorubicinZorubicin may increase the respiratory depressant activities of Cisatracurium besylate.Experimental
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB14705
KEGG Drug
D00759
PubChem Compound
62886
PubChem Substance
46506666
ChemSpider
56614
ChEBI
3721
ChEMBL
CHEMBL1200641
Therapeutic Targets Database
DAP000196
PharmGKB
PA164744925
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
AHFS Codes
  • 12:20.20 — Neuromuscular Blocking Agents
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedNot AvailableIntraocular Pressure1
3CompletedPreventionFasciculations2
3RecruitingTreatmentAcute Respiratory Distress Syndrome (ARDS)1
4CompletedNot AvailableNeuromuscular Block1
4CompletedPreventionPostoperative Residual Curarization / Residual Neuromuscular Block1
4CompletedTreatmentAcute Respiratory Distress Syndrome (ARDS)1
4Enrolling by InvitationBasic ScienceARDS, Human / Critical Illness / Neuromuscular Blockade / Paralysis / Respiratory Distress Syndrome, Adult / Respiratory Failure1
4RecruitingPreventionNeuromuscular Blockade / Postoperative Complications1
4RecruitingTreatmentIntracranial Pressure Increase / Traumatic Brain Injury (TBI)1
4Unknown StatusTreatmentAcute Respiratory Distress Syndrome (ARDS)1
4Unknown StatusTreatmentAdrenal Suppression / Hemodynamics Instability1
4Unknown StatusTreatmentAnaesthesia therapy / Hemodynamics / Oxidative Stress1
4Unknown StatusTreatmentAnalgesia, Patient-Controlled / Arthroplasty / Gastric Resection1
4Unknown StatusTreatmentPerioperative/Postoperative Complications / PORC (Postoperative Residual Curarization)1
4WithdrawnNot AvailableNeuromuscular Blockade1
Not AvailableCompletedNot AvailableGender1
Not AvailableCompletedNot AvailableNeuromuscular Blockade1
Not AvailableCompletedTreatmentAnaesthesia therapy / Chronic Otitis Media1
Not AvailableCompletedTreatmentPostoperative pain1
Not AvailableNot Yet RecruitingTreatmentNeuromuscular Blockade1
Not AvailableRecruitingNot AvailableNeuromuscular Blockade1
Not AvailableRecruitingTreatmentNeuromuscular Blockade1
Not AvailableRecruitingTreatmentPostoperative Complications1
Not AvailableRecruitingTreatmentThe Comparison of the I-gel and Endotracheal Tube About in Different Ventilation Settings During Laparoscopic Surgery1
Not AvailableTerminatedTreatmentIntubations1
Not AvailableUnknown StatusNot AvailableC.Delivery; Surgery (Previous), Gynecological1
Not AvailableUnknown StatusNot AvailablePostcardiac Arrest Therapeutic Hypothermia1

Pharmacoeconomics

Manufacturers
  • Baxter healthcare corp anesthesia and critical care
  • Baxter healthcare corp anesthesia critical care
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • Marsam pharmaceuticals llc
  • Teva parenteral medicines inc
  • Abbott laboratories
Packagers
Dosage forms
FormRouteStrength
InjectionIntravenous10 mg/mL
InjectionIntravenous2 mg/mL
Injection, solutionIntravenous10 mg/mL
Injection, solutionIntravenous2 mg/mL
SolutionIntravenous2 mg
LiquidIntravenous2 mg
LiquidIntravenous10 mg
Prices
Unit descriptionCostUnit
Nimbex 10 mg/ml vial13.8USD ml
Nimbex 2 mg/ml vial2.91USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5453510No1992-09-262012-09-26Us
CA2087104No1998-08-182011-07-12Canada

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.17e-05 mg/mLALOGPS
logP3.34ALOGPS
logP-0.96ChemAxon
logS-7.5ALOGPS
pKa (Strongest Acidic)19.02ChemAxon
pKa (Strongest Basic)-4.1ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area126.44 Å2ChemAxon
Rotatable Bond Count28ChemAxon
Refractivity280.68 m3·mol-1ChemAxon
Polarizability105.55 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9847
Blood Brain Barrier+0.9291
Caco-2 permeable-0.5966
P-glycoprotein substrateSubstrate0.6828
P-glycoprotein inhibitor IInhibitor0.7177
P-glycoprotein inhibitor IIInhibitor0.5808
Renal organic cation transporterNon-inhibitor0.5871
CYP450 2C9 substrateNon-substrate0.7994
CYP450 2D6 substrateNon-substrate0.7779
CYP450 3A4 substrateSubstrate0.6527
CYP450 1A2 substrateNon-inhibitor0.8244
CYP450 2C9 inhibitorNon-inhibitor0.7179
CYP450 2D6 inhibitorNon-inhibitor0.791
CYP450 2C19 inhibitorNon-inhibitor0.7048
CYP450 3A4 inhibitorNon-inhibitor0.7338
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8547
Ames testNon AMES toxic0.544
CarcinogenicityNon-carcinogens0.5302
BiodegradationReady biodegradable0.8169
Rat acute toxicity2.6124 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6043
hERG inhibition (predictor II)Inhibitor0.6507
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzenesulfonic acids and derivatives. These are organic compounds containing a sulfonic acid or a derivative thereof that is linked to a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzenesulfonic acids and derivatives
Direct Parent
Benzenesulfonic acids and derivatives
Alternative Parents
Benzenesulfonyl compounds / 1-sulfo,2-unsubstituted aromatic compounds / Dicarboxylic acids and derivatives / Sulfonyls / Organosulfonic acids / Organic zwitterions / Organic salts / Organic oxides / Hydrocarbon derivatives
Substituents
Benzenesulfonate / Arylsulfonic acid or derivatives / Benzenesulfonyl group / 1-sulfo,2-unsubstituted aromatic compound / Dicarboxylic acid or derivatives / Organic sulfonic acid or derivatives / Organosulfonic acid or derivatives / Organosulfonic acid / Sulfonyl / Organic oxide
Molecular Framework
Not Available
External Descriptors
quaternary ammonium salt, organosulfonate salt, atracurium besylate (CHEBI:3721)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
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
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-2
Molecular Weight
59764.82 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. Tuba Z, Maho S, Vizi ES: Synthesis and structure-activity relationships of neuromuscular blocking agents. Curr Med Chem. 2002 Aug;9(16):1507-36. [PubMed:12171561]

Drug created on June 13, 2005 07:24 / Updated on January 14, 2018 10:04