Formulation: A solid
Formal Name: 11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Purity: ≥98%
Formula Markup: C24H31N5O2
Formula Weight: 421,5
Shelf life (days): 1460
CAS Number: 102394-31-0
Notes: AF-DX 116 is an antagonist of M2 muscarinic acetylcholine receptors (Ki = 0.2 µM).{52673} It is selective for cardiac M2 over salivary gland M3 receptors (Ki = 5.01 µM) but also binds sympathetic ganglia M1 receptors (Ki = 0.81 µM). AF-DX 116 (0.1 µM) increases vagus nerve stimulation-induced increases in perfusion pressure by 50% in isolated perfused rat hearts.{52674} It increases systolic blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress when administered intravenously at doses of 50, 100, and 200 µg/kg.{52675}