Uses
AF-DX 116 has been used as an M2 muscarinic acetylcholine receptor (M2AChR) selective antagonist to study the influence of M2AChR in the regulation of both basal and carbachol-stimulated long-term potentiation at the dentate gyrus (DG-LTP) and pro-nerve growth factor (proNGF) secretion in hippocampal cells of young diabetic rats.
Definition
ChEBI: 11-[2-[2-(diethylaminomethyl)-1-piperidinyl]-1-oxoethyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one is a benzodiazepine.
Biological Activity
Selective M 2 muscarinic receptor antagonist. K i values are 64, 417, 786, 211 and 5130 nM for human recombinant M 2 , M 1 , M 3 , M 4 and M 5 muscarinic receptors, respectively.
Biochem/physiol Actions
AF-DX 116 raises blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress. Thus, it may be used as a therapeutic for hypotension related to vagotonia type autonomic dysfunction.