N-[2-[2-[(Dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide

Description

AF-DX 384 is an antagonist of M₂ and M₄ muscarinic acetylcholine receptors (K_is = 6.03 and 10 nM, respectively). It is selective for M₂ and M₄ over M₁, M₃, and M₅ receptors (K_is = 30.9, 66.07, and 537.03 nM, respectively). AF-DX 384 increases acetylcholine release in the hippocampus and cortex of young and aged rats in vivo when infused locally at a concentration of 1 μM and in the cortex when administered intraperitoneally at a dose of 5 mg/kg. It reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .

Uses

AF-DX 384 is a potent mAChR M2/mAChR M4selective antagonist.

Definition

ChEBI: N-[2-[2-[(dipropylamino)methyl]-1-piperidinyl]ethyl]-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide is a benzodiazepine.

storage

Store at RT

References

[1] F DRJE. Antagonist binding profiles of five cloned human muscarinic receptor subtypes.[J]. Journal of Pharmacology and Experimental Therapeutics, 1991, 256 2: 727-733.
[2] M.G VANNUCCHI. Selective muscarinic antagonists differentially affect in vivo acetylcholine release and memory performances of young and aged rats[J]. Neuroscience, 1997, 79 3: Pages 837-846. DOI: 10.1016/s0306-4522(97)00091-2