Receptors involved in neurotransmission are an important target for drug therapy and the identification and development of receptor-specific compounds is an essential part of contemporary drug development. Antagonists acting at detrusor muscarinic receptors and prostatic adrenergic receptors are now established therapies for the treatment of bladder instability and benign prostatic hyperplasia, respectively. Future developments await the results of basic pathophysiological studies to establish the role of classical and nonadrenergic, noncholinergic neurotransmission in the development and maintenance of diseases of the lower urinary tract. With the development of better pharmacological tools and molecular biological techniques, receptor properties are likely to be found to be tissue-specific, making the development of drugs with true tissue specificity and fewer side effects a reality.