Otilonium (bromide)

Otilonium is an inhibitor of L-type (IC50 = 2.3 µM) and T-type calcium channels (IC50s = 0.8, 1.1, and 0.4 µM for Cav3.1, Cav3.2, and Cav3.3, respectively). It is also an antagonist of muscarinic acetylcholine receptors (mAChRs, IC50s = 0.054, 0.4, 0.222, and 0.156 µM for M1, M2, M4, and M5 muscarinic receptors, respectively) and the platelet activating factor (PAF) receptor (IC50 = 0.0552 µM). Otilonium inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by the L-type calcium channel inhibitor nifedipine (Cay-11106). It inhibits contractions induced by the muscarinic acetylcholine receptor (mAChR) agonist methacholine in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 µM). Otilonium (4 mg/kg) decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of opioid withdrawal syndrome induced by morphine and naloxone.Formal Name: N,N-diethyl-N-methyl-2-[[4-[[2-(octyloxy)benzoyl]amino]benzoyl]oxy]-ethanaminium, monobromide. CAS Number: 26095-59-0. Synonyms: Octylonium. Molecular Formula: C29H43N2O4 . Br. Formula Weight: 563.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 292 nm. SMILES: O=C(NC1=CC=C(C(OCC[N+](CC)(C)CC)=O)C=C1)C2=CC=CC=C2OCCCCCCCC.[Br-]. InChi Code: InChI=1S/C29H42N2O4.BrH/c1-5-8-9-10-11-14-22-34-27-16-13-12-15-26(27)28(32)30-25-19-17-24(18-20-25)29(33)35-23-21-31(4,6-2)7-3,/h12-13,15-20H,5-11,14,21-23H2,1-4H3,1H. InChi Key: VWZPIJGXYWHBOW-UHFFFAOYSA-N.