153-76-4
Chemical Structure
Gallamine
- CAS No.: 153-76-4
- Formula:C24H45N3O3
- Molecular Weight:423.63
IUPAC Name: 2,2',2''-(benzene-1,2,3-triyltris(oxy))tris(N,N-diethylethan-1-amine)
InChIKey: ICLWTJIMXVISSR-UHFFFAOYSA-N
SMILES: CCN(CC)CCOC1=C(OCCN(CC)CC)C(OCCN(CC)CC)=CC=C1
Biological Activity: Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235 μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant[1][2].
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Gallamine | Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235 μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant. | |||||||||||||||||||||
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References
- [1]. Elsinghorst PW, et al. First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. J Med Chem. 2007 Nov 15;50(23):5685-95. [Content Brief]
- [2]. Matsuki A, et al. Effect of gallamine on plasma cortisol and catecholamine levels in man. Can Anaesth Soc J. 1973 Jul;20(4):539-45. [Content Brief]
