The binding of (3H)-propylbenzilycholine mustard by longitudinal muscle strips from guinea-pig small intestine.
1 The synthesis of tritium labelled propylbenzilylcholine mustard ([(3)H]-PrBCM; N-2'-chloroethyl-N-[2'', 3''-(3)H(2)] propyl-2-aminoethyl benzilate) is described.2 The uptake by muscle strips was measured and shown to be considerably increased by previous immersion of the muscle in distilled water.3 A considerable part of the uptake is inhibited selectively by atropine, but not by nicotinic antagonists. A number of muscarinic agonists also inhibit uptake and their apparent affinity constants have been determined.4 The uptake by atropine-sensitive sites is temperature-insensitive, whereas the other sites are temperature-sensitive. Recovery is highly temperature-sensitive and there is good agreement between recovery of sensitivity to agonists and loss of radioactivity from the muscle.
D000477:Alkylating Agents / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000378:metabolism*; D000818:Animals; D001285:Atropine / Q000032:analysis / Q000494:pharmacology; D001561:Benzilates / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000378:metabolism; D001665:Binding Sites / Q000187:drug effects; D002794:Choline / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000378:metabolism*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007421:Intestine, Small; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000378:metabolism*; D009150:Mustard Compounds / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000378:metabolism*; D009388:Neostigmine / Q000494:pharmacology; D010830:Physostigmine / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology; D011955:Receptors, Drug; D013696:Temperature; D013997:Time Factors; D014316:Tritium; D014867:Water
D000477:Alkylating Agents; D001561:Benzilates; D009150:Mustard Compounds; D000644:Quaternary Ammonium Compounds; D011955:Receptors, Drug; D014867:Water; D014316:Tritium; D009388:Neostigmine; D001285:Atropine; D010830:Physostigmine; D002794:Choline