methoctramine

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]

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

LASSBio-873, an orally active muscarinic cholinergic receptor (mAChR) agonist, is capable of crossing the blood-brain barrier. It exhibits potent analgesic effects on acute and inflammatory pain, which can be inhibited by the intrathecal injection of the M2 receptor antagonist methoctramine [1].