In the present study, two 6-(fluorobenzoyl)-3-piperazinomethyl-2benzothiazo
line ne derivatives were synthesized and their relaxant effects on isolated
rabbit corpus cavernosum investigated. Compounds Y-16 and Y-21 can alter t
he ability of corpus cavernosum smooth muscle to contract. Strips of rabbit
corpus cavernosum smooth muscle were mounted in isolated tissue baths for
measurement of isometric contractile force. Compounds (10(-6)-10(-3) M) did
not cause contraction but induced relaxation in precontracted corpus caver
nosum smooth muscle. Neither N-nitro-L-arginine methylester (L-NAME) nor in
domethacin affected the relaxant effect of these compounds. Glibenclamide a
nd tetraethylammonium chloride (TEA) also did not influence the relaxation
induced by the compounds. In conclusion, in isolated rabbit corpus cavenosu
m, Y16 and Y21 have a relaxant potency equal or superior to known vasoactiv
e agents. Further investigations are needed to show the importance of these
effects for the diagnosis and treatment of erectile dysfunction.