Abstract: The invention relates to the treatment of sexual dysfunction by inhibition of vasoconstriction leading to the relaxation of smooth muscles in male or female erectile tissue. In one aspect, the invention comprises methods for treating male and female sexual dysfunction which comprises administering a composition comprising a compound which attenuates RhoA and/or Rho-kinase activity in an organ subject to sexual stimulation in a pharmaceutically acceptable carrier to an individual in need of such treatment. In one embodiment, the compound comprises an inhibitor of the enzyme Rho-kinase. In other embodiments, compounds targeted to other enzymes involved in phosphorylation of myosin light chain are used. Also described are compositions and kits for performing the methods of the invention.