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Abstract

Comparative studies of substrates and inhibitors of choline transport and choline acetyltransferase.

L A Barker and T W Mittag
Journal of Pharmacology and Experimental Therapeutics January 1975, 192 (1) 86-94;
L A Barker
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T W Mittag
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Abstract

Analogs of choline and three hemicholinium derivatives were studied as substrates for choline acetyltransferase (ChAc) and as substrates or inhibitors of the high-affinity choline transport system in rat brain synaptosomes. Hemicholiniums-3 and -15, but not terphenylhemicholinium-3, were substrates of ChAc. All three inhibit the high-affinity choline transport system, with I50 values of 0.08, 8.0 and 0.08 muM, respectively. Simple choline analogs with substituents on the beta-carbon atom were found to be very poor substrates for ChAc. N-alkyl analogs, mono-, di- and triethyl choline and N-hydroxyethyl pyrrolidinium methiodide (pyrrolcholine), and DL-alpha-methyl choline are substrates for ChAc and also inhibit choline transport, with I50 values between 2 to 6 muM.[3-H] choline, [3-H] monoethycholine and [3-H] pyrrolcholine were transported into synaptosomes by the choline high affinity system and metabolized to acetyl derivatives. The results indicated that choline transport is the rate-limiting step in the biosynthesis of acetylcholine and provide the basis for the development of a group of cholinergic false transmitters.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 192, Issue 1
1 Jan 1975
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Abstract

Comparative studies of substrates and inhibitors of choline transport and choline acetyltransferase.

L A Barker and T W Mittag
Journal of Pharmacology and Experimental Therapeutics January 1, 1975, 192 (1) 86-94;

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Abstract

Comparative studies of substrates and inhibitors of choline transport and choline acetyltransferase.

L A Barker and T W Mittag
Journal of Pharmacology and Experimental Therapeutics January 1, 1975, 192 (1) 86-94;
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