A muscarinic M2 receptor antagonist (Ki = 0.2 µM); selective for cardiac M2 over salivary gland M3 receptors (Ki = 5.01 µM) but also binds sympathetic ganglia M1 receptors (Ki = 0.81 µM); increases vagus nerve stimulation-induced increases in perfusion pressure by 50% in isolated perfused rat hearts at 0.1 µM; increases systolic blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress at 50

AF-DX 116 – 1 mg

Brand:
Cayman
CAS:
102394-31-0
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A muscarinic M2 receptor antagonist (Ki = 0.2 µM); selective for cardiac M2 over salivary gland M3 receptors (Ki = 5.01 µM) but also binds sympathetic ganglia M1 receptors (Ki = 0.81 µM); increases vagus nerve stimulation-induced increases in perfusion pressure by 50% in isolated perfused rat hearts at 0.1 µM; increases systolic blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress at 50, 100, and 200 µg/kg

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

Synonyms: 

Molecular weight: 421.5

CAS: 102394-31-0

Purity: ≥98%

Formulation: A solid

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