Portal de Periódicos da CAPES

Chapter 6. Progress in the Development of Neurokinin Antagonists

1999; Elsevier BV; Linguagem: Inglês

10.1016/s0065-7743(08)60568-0

1557-8437

Christopher J. Swain, N.M.J. Rupniak,

Pain Mechanisms and Treatments

This chapter focuses on the progress in the development of neurokinin (NK) antagonists. The neurokinins substance P (SP), neurokinin A (NKA), and neurokinin B (NKB) are related neuropeptides that are widely distributed in the peripheral and central nervous systems (CNS). With the recent development of highly selective nonpeptide antagonists of these receptors, it has become possible to investigate the physiological roles of these peptides. The vast majority of these compounds are selective SP antagonists, however a number of selective NKA and NKB antagonists have been reported. NK receptor antagonists have potential for the treatment of a wide variety of medical disorders. Preclinical findings suggest the use of NK antagonists in a diverse range of therapeutic indications, including, migraine, arthritis, pain, and inflammatory diseases such as cystitis. Other indications include, inflammatory bowel disease, and other gastric disorders, in particular cancer chemotherapy induced emesis, asthma, anxiety and depression, and cancer. The chapter presents an overview of NK1 receptor antagonists and elaborates its preclinical biology. Details of NK2 receptor antagonists are provided and clinical studies are also reviewed.