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Molecular Pharmacology, Vol 12, 769-777, Copyright © 1976 by the American Society for Pharmacology and Experimental Therapeutics

Reversible Binding of Chlorpromazine to Brain Tubulin

NORMAN D. HINMAN 1 and JOHN R. CANN 1

1 Department of Biophysics and Genetics, University of Colorado Medical Center, Denver, Colorado 80220

Chlorpromazine binds reversibly to brain tubulin via two well-resolved processes. One chlorpromazine molecule binds strongly compared with 8-9 molecules that bind weakly. Binding to the higher-affinity site is chiefly entropy-driven, implicating hydrophobic forces. The two binding processes are compared with the biological activities of chlorpromazine in vitro.

Note:
ACKNOWLEDGMENT The authors thank Mr. Robert O. Coombs for technical assistance.

Submitted on December 9, 1975
Accepted on April 6, 1976






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