1 Ginsenosides, the active ingredients extracted from Panax ginseng, have been shown to promote nitric oxide (NO) release in bovine aortic endothelial cells. Since the endothelial cells and the perivascular nerves in penile corpus cavernosum contain NO synthase and an NO-like substance has been shown to be released from these cells which relaxes corpus cavernosum the possibility that ginsenosides may relax corpus cavernosum by releasing endogenous NO was examined. 2 With an in vitro tissue superfusion technique, ginsenosides (250, 500 and 750 mu g ml(-1)) relaxed corpus cavernosum, concentration-dependently. 3 Using an in vitro tissue bath technique, acetylcholine (ACh)-induced relaxations were increased in the presence of ginsenosides (250 mu g ml(-1)). 4 Ginsenosides at 100 mu g ml(-1) significantly enhanced the tetrodotoxin (TTX)-sensitive relaxation of corpus cavernosum elicited by transmural nerve stimulation. 5 The ginsenosides-induced, ACh-induced and ginsenosides-enhanced transmural nerve stimulation-elicited relaxations were significantly attenuated by N-G-nitro-L-arginine (100 mu M) and oxyhaemoglobin (oxyHb; 5-10 mu M), and were enhanced by superoxide dismutase (SOD; 50 u ml(-1)). 6 The relaxations and their attenuation by N-G-nitro-L-arginine and TTX were associated with increase and decrease in tissue cyclic GMP levels, respectively. 7 It is concluded that ginsenosides may release NO from endothelial cells, and enhance NO release from endothelial cells elicited by other vasoactive substances and from perivascular nitrergic nerves in the corpus cavernosum. These endothelial and neurogenic effects of ginsenosides in inducing relaxation of the corpus cavernosum may account for the aphrodisiac effect of Panax ginseng.