Muscarinic receptor antagonists remain the main therapy for the treatment o
f the overactive bladder yet severe adverse effects make them unsuitable fo
r a large number of patients. The development of new drugs with novel mecha
nisms of action for the treatment of this condition is therefore essential.
This article considers some of the targets currently under investigation f
or the development of such compounds. beta -adrenoceptor agonists and K-ATP
channel openers inhibit detrusor muscle activity and remain targets for dr
ug development. There is also evidence that alpha -adrenoceptor antagonists
may be effective in the overactive bladder, but the mechanism involved in
this action is unclear. Finally the role of tachykinins in regulating bladd
er function through both the sensory and the motor innervation make them a
potential target for drug development, but as with the the others, a select
ive action on the bladder must remain the goal of drug development.