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(Des-Histidine1) (Nϵ-phenylthiocarbamoyllysine12)-glucagon: Effects on glycogenolysis in perfused rat liver
Authors:B.A. Khan  Marvin D. Bregman  C.A. Nugent  Victor J. Hruby  K. Brendel
Affiliation:1. Department of Pharmacology, Arizona Health Sciences Center, University of Arizona, Tucson, Arizona 85721 USA;7. Department of Internal Medicine, Arizona Health Sciences Center, University of Arizona, Tucson, Arizona 85721 USA;71. the Department of Chemistry, University of Arizona, Tucson, Arizona 85721 USA
Abstract:(Des-Histidine1) (N?-phenylthiocarbamoyllysine12)-glucagon, synthesized by the one-step Edman degradation procedure is a competitive inhibitor of glucagon action in the rat liver plasma membrane adenylate cyclase system. However, in the perfused rat liver, the compound did not inhibit glucagon stimulated glycogenolysis even when used at a concentration 100-fold in excess of native glucagon. Instead, it showed a weak potency, but full agonist activity, stimulating liver glycogenolysis to 100% of the level obtained by glucagon. These results are discussed in terms of the possible mechanism(s) of glucagon action.
Keywords:To whom correspondence and reprint requests should be sent.
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