The effect of the experimental antitumor agent caracemide on brain choline acetyltransferase | Zendy

Ho B. T. | Zendy; Tansey L. W. | Zendy; Feiffer R. | Zendy; Newman R. A. | Zendy; Farquhar D. | Zendy; Field W. S. | Zendy; Krakoff I. H. | Zendy

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The effect of the experimental antitumor agent caracemide on brain choline acetyltransferase

Author(s) -

Ho B. T.,

Tansey L. W.,

Feiffer R.,

Newman R. A.,

Farquhar D.,

Field W. S.,

Krakoff I. H.

Publication year - 1988

Publication title -

journal of neuroscience research

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.72

H-Index - 160

eISSN - 1097-4547

pISSN - 0360-4012

DOI - 10.1002/jnr.490190116

Subject(s) - choline acetyltransferase , acetylcholine , choline , substrate (aquarium) , acetamide , chemistry , enzyme , mixed inhibition , inhibitory postsynaptic potential , non competitive inhibition , stereochemistry , biochemistry , pharmacology , biology , endocrinology , organic chemistry , ecology

Caracemide was found to inhibit choline acetyltransferase (CAT) from rat brain. A concentration of 0.5 mM caracemide inhibited the enzyme by 93%, whereas a degradation product from caracemide, N‐(methycarbamoyloxy)acetamide, produced only a 50% inhibition. Two other degration products, N(methyl‐carbamoyloxy)‐N′‐methylurea and N‐hydroxy‐N′‐methlurea, lacked any inhibitory activity. With bovine brain CAT, caracemide showed noncompetitive inhibitio with the substrate choline, K m 337 μM, K i μM, V max 2.83 nmol acetylcholine fromed/ mg/mg protein and mixed inhibition with the substrate acetyl‐CoA, K m 21 μM, K i 146 μM, V max 3.85 noml acetylcholine formed/min/mg porotein.

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