methoctramine

Methoctramine tetrahydrochloride is a potent and cardioselective antagonist of the M2 muscarinic receptor, capable of inhibiting Muscarine-induced bradycardia in vivo.

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] 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.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein 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.[3]

LASSBio-873是一种强效高选择性的 5-HT4 激动剂。它在动物模型中表现出显著的促动力活性并能改善认知功能，常用于胃肠道蠕动障碍及阿尔茨海默病相关的记忆增强研究。