Отилония бромид

Описание

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 Ca_v3.1, Ca_v3.2, and Ca_v3.3, 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 . 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.

Химические свойства

White Powder

Использование

Otilonium bromide is an antimuscarinic

Общее описание

Otilonium bromide is an antispasmodic. It contains a red color ACh (acetylcholine) like moiety bound to an aromatic system that ends with an octyl ether.

Профиль безопасности

Poison by intraperitoneal route. Moderately toxic by ingestion and subcutaneous routes. When heated to decomposition it emits toxic fumes of Brí and NOx.