AF-DX 116 discriminates between muscarinic M2 receptors of the heart and vasculature.
The newly developed muscarinic antagonist, AF-DX 116, has been reported to have a higher affinity in vivo for muscarinic receptors in the heart than in the vasculature. Therefore two in vitro preparations, the rabbit ear artery and spontaneously beating right atrium, were compared. AF-DX 116 had a 29 times greater affinity for muscarinic receptors in the cardiac preparation than in the ear artery, with a pA2 in the heart of 7.42 compared to a value of 5.95 in the ear artery. Thus AF-DX 116 shows promise as an approach to differentiating sub-classes of muscarinic M2 receptors.
D000818:Animals; D001158:Arteries / Q000502:physiology; D016275:Atrial Function; D004423:Ear / Q000098:blood supply; D005260:Female; D008297:Male; D009126:Muscle Relaxation / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000502:physiology*; D009200:Myocardial Contraction / Q000187:drug effects*; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000494:pharmacology; D011817:Rabbits; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000502:physiology*
D011976:Receptors, Muscarinic; D010890:Pirenzepine; C048593:otenzepad