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Methoctramine (CAS 104807-46-7)

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Alternate Names:
Methoctramine tetrahydrochloride
Application:
Methoctramine is a mAChR M2 (muscarinic M2 receptor) antagonist
CAS Number:
104807-46-7
Purity:
≥97%
Molecular Weight:
728.75
Molecular Formula:
C36H62N4O24HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Methoctramine is a highly selective antagonist for cardiac mAChR M2 (M2 muscarinic receptors), which are involved in reducing heart rate after stimulatory actions of the parasympathetic nervous system. At nanomolar concentrations, Methoctramine may act to strongly inhibit bradychardia induced by both vagal stimulation and acetylcholine. Methoctramine has low affinity for M1 receptors and non-cardiac M2 receptors.


Methoctramine (CAS 104807-46-7) References

  1. Effects of methoctramine on bladder overactivity in a rat model.  |  Ozturk, H., et al. 2003. Urology. 61: 671-6. PMID: 12639681
  2. Methoctramine, a cardioselective antagonist: muscarinic receptor mediating prostaglandin synthesis in isolated rabbit heart.  |  Jaiswal, N. and Malik, KU. 1991. Eur J Pharmacol. 192: 63-70. PMID: 1904033
  3. Cytotoxicity of methoctramine and methoctramine-related polyamines.  |  Zini, M., et al. 2009. Chem Biol Interact. 181: 409-16. PMID: 19576191
  4. Molecular mechanisms of methoctramine binding and selectivity at muscarinic acetylcholine receptors.  |  Jakubík, J., et al. 2014. Mol Pharmacol. 86: 180-92. PMID: 24870405
  5. Different mechanisms of antagonism by methoctramine of two neuronal muscarinic receptor-mediated second messenger responses.  |  Lee, NH., et al. 1989. J Pharmacol Exp Ther. 251: 992-9. PMID: 2557423
  6. Methoctramine, a selective M2 alpha muscarinic receptor antagonist, does not inhibit carbachol-induced drinking in the rat.  |  Massi, M., et al. 1989. Eur J Pharmacol. 163: 387-91. PMID: 2721580
  7. Methoctramine selectively blocks cardiac muscarinic M2 receptors in vivo.  |  Wess, J., et al. 1988. Naunyn Schmiedebergs Arch Pharmacol. 338: 246-9. PMID: 3057387
  8. The interaction of methoctramine and himbacine at atrial, smooth muscle and endothelial muscarinic receptors in vitro.  |  Eglen, RM., et al. 1988. Br J Pharmacol. 95: 1031-8. PMID: 3219478
  9. Antimuscarinic action of methoctramine, a new cardioselective M-2 muscarinic receptor antagonist, alone and in combination with atropine and gallamine.  |  Melchiorre, C., et al. 1987. Eur J Pharmacol. 144: 117-24. PMID: 3436364
  10. Methoctramine induces nonspecific airway hyperresponsiveness in vivo.  |  Howell, RE., et al. 1994. Eur J Pharmacol. 265: 67-75. PMID: 7883031
  11. Methoctramine binding sites sensitive to alkylation on muscarinic receptors from tracheal smooth muscle.  |  Misle, AJ., et al. 1994. Biochem Pharmacol. 48: 191-5. PMID: 8043022
  12. Postsynaptic effects of methoctramine at the mouse neuromuscular junction.  |  Re, L., et al. 1993. Neuroscience. 57: 451-7. PMID: 8115049
  13. Methoctramine moderately improves memory but pirenzepine disrupts performance in delayed non-matching to position test.  |  Aura, J., et al. 1997. Eur J Pharmacol. 333: 129-34. PMID: 9314025

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Methoctramine, 10 mg

sc-257709
10 mg
$306.00

Methoctramine, 25 mg

sc-257709A
25 mg
$444.00