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W. LEIDL and W. BIERGERT

Summary.

The cutaneous absorption of penicillin dissolved in DMSO and penicillin dissolved in water were compared following topical application to the testis of two boars and two bulls. DMSO demonstrated pharmacodynamic activities, which suggests that further study of its activity by topical application in the therapy of epididymal and testicular diseases is indicated.

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W. Müller-Esterl, V. Wendt, W. Leidl, O. Dann, E. Shaw, G. Wagner and H. Fritz

Summary. Thirteen serine proteinase inhibitors of the guanidine, monoamidine and diamidine type were tested for their ability to inhibit the proteinase acrosin present in the acrosome of ejaculated and capacitated boar spermatozoa. All compounds studied proved to be potent in-vitro inhibitors of acrosin. Inhibition constants (Ki) in the range of 1·2 × 10−7 to 6 × 10−8 M were found for the reversible inhibitors. The intra-acrosomal inhibition of acrosin was assessed by the gelatin substrate film method: 2 guanidinobenzoates, one monoamidine and one diamidine derivative proved to inhibit acrosin completely in intact spermatozoa. Intravenous injection of 6-amidino-2-(4-amidinophenyl)-indole had no effect on fertilization, but application of 4-nitrophenyl-4-guanidinobenzoate in a vaginal suppository gave a 50% reduction of fertilization.