Methoctramine |
| رقم الكتالوجGC18563 |
ميثوكترامين هو مضاد قوي وانتقائية للقلب لمستقبلات M2 المسكارينية.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 104807-46-7
Sample solution is provided at 25 µL, 10mM.
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).
| 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 |
| الذوبان | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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