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Methoctramine

Catalog No.GC18563

La méthoctramine est un antagoniste puissant et cardiosélectif du récepteur muscarinique M2.

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Methoctramine Chemical Structure

Cas No.: 104807-46-7

Taille Prix Stock Qté
5mg
162,00 $US
En stock
10mg
293,00 $US
En stock
25mg
564,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Description Chemical Properties Product Documents Related Products

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 uM. [2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholine in 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] 

Reference
[1]. Buckley, N.J., Bonner, T.I., Buckley, C.M., et al. Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells. Mol. Pharm. 35(4), 469-476 (1989).
[2]. Watson, N., Barnes, P.J., and Maclagan, J. Actions of methoctramine, a muscarinic M2 receptor antagonist, on muscarinic and nicotinic cholinoceptors in guinea-pig airways in vivo and in vitro. Br. J. Pharmacol. 105(1), 107-112 (1992).
[3]. Matsumoto, Y., Miyazato, M., Yokoyama, H., et al. Role of M2 and M3 muscarinic acetylcholine receptor subtypes in activation of bladder afferent pathways in spinal cord injured rats. Urology 79(5), 1184.e1115-e1120 (2012).

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