An L- and T-type calcium channel inhibitor (IC50s = 2.3

Otilonium (bromide) – 50 mg

Brand:
Cayman
CAS:
26095-59-0
Storage:
-20
UN-No:
Non-Hazardous - /

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).{46774,46775} 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).{46778} 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 (Item No. 11106).{46774} 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).{46776} 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.{46777}  

 

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Description

An L- and T-type calcium channel inhibitor (IC50s = 2.3, 0.8, 1.1, and 0.4 µM for Cav1.2, Cav3.1, Cav3.2, and Cav3.3, respectively) and mAChR antagonist (IC50s = 0.054, 0.4, 0.222, and 0.156 µM for M1, M2, M4, and M5 muscarinic receptors, respectively); inhibits the PAF receptor (IC50 = 0.0552 µM); inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by an L-type calcium channel inhibitor; inhibits mAChR agonist-induced contractions in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 µM); decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of morphine- and naloxone-induced opioid withdrawal syndrome at 4 mg/kg

Formal name: N,N-diethyl-N-methyl-2-[[4-[[2-(octyloxy)benzoyl]amino]benzoyl]oxy]-ethanaminium, monobromide

Synonyms:  Octylonium

Molecular weight: 563.6

CAS: 26095-59-0

Purity: ≥98%

Formulation: A crystalline solid

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