Cisatracurium (besylate)

Cisatracurium is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) and non-depolarizing muscle relaxant. It inhibits stimulation of human adult muscle nAChRs by acetylcholine (Cay-23829) with an IC50 value of 10 nM. It also inhibits mouse nAChRs with IC50 values of 54 and 115 nM for adult and embryonic receptors, respectively. Cisatracurium increases apoptosis in HUVEC cells and decreases proliferation of HepG2 and HUVEC cells in vitro in a concentration-dependent manner. It reduces the magnitude of electrically-evoked twitch tensions in isolated rat extensor digitorum longus and soleus sciatic nerve muscle preparations in a dose-dependent manner. Cisatracurium blocks electrically-evoked muscle twitches in anesthetized rabbits with an ED95 value of 0.04 mg/kg. Formulations containing cisatracurium have been used to facilitate intubation prior to surgery and as muscle relaxants.Formal Name: (1R,1'R,2R,2'R)-2,2'-[1,5-pentanediylbis[oxy(3-oxo-3,1-propanediyl)]]bis[1-[(3,4-dimethoxyphenyl)methyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-isoquinolinium, dibenzenesulfonate. CAS Number: 96946-42-8. Molecular Formula: C53H72N2O12 . 2C6H5O3S. Formula Weight: 1243.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 280 nm. SMILES: COC1=C(OC)C=C(C[C@@H]2C(C=C(OC)C(OC)=C3)=C3CC[N@+]2(C)CCC(OCCCCCOC(CC[N@@+]4(C)CCC(C=C(OC)C(OC)=C5)=C5[C@H]4CC6=CC(OC)=C(OC)C=C6)=O)=O)C=C1.[O-]S(C7=CC=CC=C7)(=O)=O.[O-]S(C8=CC=CC=C8)(=O)=O. InChi Code: 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. InChi Key: XXZSQOVSEBAPGS-DONVQRBFSA-L.