Human erythrocyte as a model for investigating muscarinic agonists and antagonists.
1. Human erythrocyte muscarinic receptor is further classified as M1 subtype by its binding of [3H]pirenzepine (a specific M1 antagonist). Conversely, binding of [3H]piperidinyl AF-DX116 (a specific M2 antagonist) is not detected. 2. There are high correlations between the binding efficacies of 25 known or putative cholinergic agents using either human erythrocyte membrane or mouse caudate homogenate. Also the in vitro data corresponds satisfactorily with in vivo data measuring the protective effect of these compounds against organophosphate poisoning. 3. The human erythrocyte membrane is an efficient model for investigating cholinergic agonists and antagonists.
Tang
L C
LC
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, DC 20307.
D000818:Animals; D001921:Brain / Q000187:drug effects; D002421:Caudate Nucleus / Q000187:drug effects; D004910:Erythrocyte Membrane / Q000187:drug effects; D004912:Erythrocytes / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008954:Models, Biological; D010276:Parasympatholytics / Q000494:pharmacology* / Q000633:toxicity; D010277:Parasympathomimetics / Q000494:pharmacology* / Q000633:toxicity; D010890:Pirenzepine / Q000031:analogs & derivatives / Q000494:pharmacology; D011813:Quinuclidinyl Benzilate / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000187:drug effects
D010276:Parasympatholytics; D010277:Parasympathomimetics; D011976:Receptors, Muscarinic; D010890:Pirenzepine; D011813:Quinuclidinyl Benzilate; C048593:otenzepad