Abstract
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.
MeSH terms
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Alkylating Agents / antagonists & inhibitors
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Alkylating Agents / chemical synthesis
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Alkylating Agents / metabolism*
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Animals
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Atropine / analysis
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Atropine / pharmacology
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Benzilates / antagonists & inhibitors
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Benzilates / chemical synthesis
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Benzilates / metabolism
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Binding Sites / drug effects
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Choline / antagonists & inhibitors
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Choline / chemical synthesis
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Choline / metabolism*
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Guinea Pigs
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In Vitro Techniques
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Intestine, Small
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Muscle Contraction / drug effects
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Muscle, Smooth / metabolism*
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Mustard Compounds / antagonists & inhibitors
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Mustard Compounds / chemical synthesis
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Mustard Compounds / metabolism*
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Neostigmine / pharmacology
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Physostigmine / pharmacology
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Quaternary Ammonium Compounds / pharmacology
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Receptors, Drug
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Temperature
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Time Factors
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Tritium
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Water
Substances
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Alkylating Agents
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Benzilates
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Mustard Compounds
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Quaternary Ammonium Compounds
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Receptors, Drug
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Water
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Tritium
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Neostigmine
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Atropine
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Physostigmine
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Choline