Treatment of erectile dysfunction without causing undesirable side-effects, using phosphodiesterase IV inhibitor, optionally in combination with other phosphodiesterase inhibitor or adenylate cyclase stimulant

摘要

A medicament for the treatment of sexual dysfunction contains a phosphodiesterase IV inhibitor (I), optionally in combination with other phosphodiesterase inhibitors (II) or adenylate cyclase stimulants (III). An independent claim is included for the use of adenylate cyclase inhibitors (optionally in combination with phosphodiesterase inhibitors) for the treatment of erectile dysfunction. ACTIVITY : Vasotropic. MECHANISM OF ACTION : Phosphodiesterase IV inhibitor; adenylate cyclase inhibitor. (I) increase the intracellular cyclic adenosine monophosphate (cAMP) level by inhibiting hydrolysis and stimulating formation; this induces an increase in cyclic guanosine monophosphate (cGMP) level by 'cross talk' and thus causes relaxation of the corpus cavernosum. Rolipram (Ia) caused relaxation of human corpus cavernosum by ca. 10% at 0.1 MicroM, 20% at 1 MicroM, 30% at 10 MicroM and 50% at 100 MicroM (i.e. IC50 was ca. 100 MicroM).