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Methoctramine

Catalog No.GC18563

Methoctramine is a potent and cardioselectivity antagonist of M2 muscarinic receptor.

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Methoctramine Chemical Structure

Cas No.: 104807-46-7

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5mg
$162.00
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10mg
$293.00
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25mg
$564.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Background

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).

Chemical Properties

Cas No. 104807-46-7 SDF
Chemical Name N1,N8-bis[6-[[(2-methoxyphenyl)methyl]amino]hexyl]-1,8-octanediamine, tetrahydrochloride
Canonical SMILES COC1=C(CNCCCCCCNCCCCCCCCNCCCCCCNCC2=C(OC)C=CC=C2)C=CC=C1.Cl.Cl.Cl.Cl
Formula C36H62N4O2.4HCl M.Wt 728.8
Solubility 10 mg/ml in PBS (pH 7.2) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.3721 mL 6.8606 mL 13.7212 mL
5 mM 0.2744 mL 1.3721 mL 2.7442 mL
10 mM 0.1372 mL 0.6861 mL 1.3721 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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