Selective and competitive M2 muscarinic receptor antagonist. Selective for M2 over M3 (Ki values are 64 and 786 nM respectively). Shows selectivity for cardiac muscarinic receptors. Shows hypertensive actions and increases heart rate in cold-stressed rats.
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References for AF-DX 116
Binding profile of a novel cardioselective muscarine receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat.
Hammer R et al (1986)Life Sci 38(18) : 1653-62.
PubMedID: 3754610
Blood pressure and heart rate are increased by AF-DX 116, a selective M2 antagonist, in autonomic imbalanced and hypotensive rats caused by repeated cold stress.
Hata T et al (2001)Jpn J Pharmacol 85(3) : 313-21.
PubMedID: 11325025
BK channel β1 subunits regulate airway contraction secondary to M2 muscarinic acetylcholine receptor mediated depolarization.
Semenov I et al (2011)J Physiol 589(Pt 7) : 1803-17.
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