104807-40-1
Chemical Structure
Methoctramine
- CAS No.: 104807-40-1
- Formula:C36H62N4O2
- Molecular Weight:582.90
IUPAC Name: N1,N1'-(octane-1,8-diyl)bis(N6-(2-methoxybenzyl)hexane-1,6-diamine)
InChIKey: RPMBYDYUVKEZJA-UHFFFAOYSA-N
SMILES: COC1=CC=CC=C1CNCCCCCCNCCCCCCCCNCCCCCCNCC2=CC=CC=C2OC
Biological Activity: Methoctramine is an M2 subtype-preferring muscarinic acetylcholine receptor (mAChR) antagonist. Methoctramine blocks presynaptic inhibitory M2 autoreceptors, relieves negative feedback inhibition, increases acetylcholine release, and enhances neuromuscular transmission. Methoctramine can be used in research on amyotrophic lateral sclerosis, breast cancer, central cholinergic hypertension, and psychostimulant use disorder[1][2][3][4][5][6].
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Methoctramine | Methoctramine is an M2 subtype-preferring muscarinic acetylcholine receptor (mAChR) antagonist. Methoctramine blocks presynaptic inhibitory M2 autoreceptors, relieves negative feedback inhibition, increases acetylcholine release, and enhances neuromuscular transmission. Methoctramine can be used in research on amyotrophic lateral sclerosis, breast cancer, central cholinergic hypertension, and psychostimulant use disorder. | |||||||||||||||||||||
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References
- [1]. de la Torre E, et al. Muscarinic receptors participation in angiogenic response induced by macrophages from mammary adenocarcinoma-bearing mice. Breast Cancer Research. 2005 Mar 4;7(3):R345. [Content Brief]
- [2]. Dobryakova YV, et al. Administration of muscarinic antagonists induce changes in passive avoidance learning and in synaptic transmission in the CA1 area of the hippocampus. Acta neurobiologiae experimentalis. 2018;78(2):132-139.
- [3]. Ozkutlu U, et al. Central muscarinic M2 cholinoceptors involved in cholinergic hypertension. European journal of pharmacology. 1993 Dec 21;250(3):349-54.
- [4]. Xu ZP, et al. Role of M3 mAChR in in vivo and in vitro models of LPS-induced inflammatory response. International immunopharmacology. 2012 Nov;14(3):320-7.
- [5]. Jakubík J, et al. Molecular mechanisms of methoctramine binding and selectivity at muscarinic acetylcholine receptors. Molecular pharmacology. 2014 Aug 1;86(2):180-92.
- [6]. Joseph L, et al. Effects of muscarinic receptor antagonists on cocaine discrimination in wild-type mice and in muscarinic receptor M1, M2, and M4 receptor knockout mice. Behav Brain Res. 2017 Jun 30;329:75-83.
