AF-DX 116

AF-DX 116 is an antagonist of M2 muscarinic acetylcholine receptors (Ki = 0.2 µM).1 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.2 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.3WARNING This product is not for human or veterinary use.

A muscarinic M2 receptor antagonist

421.5

≥98%

Biochemicals/Receptor Pharmacology/Antagonists

Formal_Name:11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one

O=C1NC(C=CC=N2)=C2N(C(CN3CCCCC3CN(CC)CC)=O)C4=C1C=CC=C4

C24H31N5O2

102394-31-0

≥ 4 years

DMSO: Soluble: =10 mg/ml Ethanol: Sparingly soluble: 1-10 mg/ml