General pharmacological effects of TZP-4238, a new antiandrogen, on central nervous and motor systems were studied. 1) At a dose of 100 mg/kg, p.o., TZP-4238 produced mild depression (slight lowering of spontaneous movement and passive state) in mice. At a dose of 300 mg/kg, p.o. and above, it induced several excitatory symptoms such as scratching, tremor (300 mg/kg), Straub's tail, twitches and
... [Show full abstract] convulsions (1000 mg/kg, lethal dose) in mice. 2) TZP-4238 at a dose of 100 mg/kg, p.o. significantly potentiated oxotremorine-induced tremor in mice. 3) TZP-4238 at a dose of 100 mg/kg, p.o. reduced acetic acid-induced writhing but did not inhibit nociceptive response against tail pressure in mice. 4) TZP-4238 at a dose of 100 mg/kg, p.o. had no effects on motor (exploratory) activity, hexobarbital-induced hypnosis, electroshock-, pentylenetetrazole- and strychnine-induced convulsions, methamphetamine-induced hyperactivity, motor coordination in mice and body temperature in rats and did not show muscle relaxing and taming effects in mice. 5) TZP-4238 at a dose of 10 mg/kg, i.v. had no effects on spinal reflex potentials in cats and ex vivo neuromuscular transmission in rats. 6) TZP-4238 at a dose of 100 mg/kg, p.o. showed potentiation of carrageenin induced rat paw edema at only 2 hours after carrageenin. 7) TZP-4238 at a dose of 100 mg/kg, p.o. did not produce any gastric damages in rats. 8) TZP-4238 had no effect on platelet retention rate in rats (100 mg/kg, p.o.) and did not influence on ADP- and collagen-induced guinea-pig platelet aggregations (1 x 10-4g/ml).