Methoctramine (hydrate)

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes). It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 µM. In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholine (Cay-23829) in guinea pigs with ED50 values of 38 and 81 nmol/kg, respectively. In a rat model of spinal cord injury, methoctramine suppresses bladder overactivity induced by the non-selective muscarinic acetylcholine receptor agonist oxotremorine M (Cay-20847).Formal Name: N1,N8-bis[6-[[(2-methoxyphenyl)methyl]amino]hexyl]-1,8-octanediamine, tetrahydrochloride, hydrate. Molecular Formula: C36H62N4O2 . 4HCl [XH2O]. Formula Weight: 728.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 10 mg/ml. lambdamax: 220, 275 nm. SMILES: COC1=C(CNCCCCCCNCCCCCCCCNCCCCCCNCC2=C(OC)C=CC=C2)C=CC=C1.Cl.Cl.Cl.Cl.O. InChi Code: InChI=1S/C36H62N4O2.4ClH.H2O/c1-41-35-23-13-11-21-33(35)31-39-29-19-9-7-17-27-37-25-15-5-3-4-6-16-26-38-28-18-8-10-20-30-40-32-34-22-12-14-24-36(34)42-2,,,,,/h11-14,21-24,37-40H,3-10,15-20,25-32H2,1-2H3,4*1H,1H2. InChi Key: UXAJCHUHTUCCCM-UHFFFAOYSA-N.