Neurokinin receptor antagonists.
Studies on tachykinin peptides and the corresponding neurokinin receptors (NKr) have increased dramatically recently due to the discovery of selective, orally-active, metabolically stable and sometimes CNS penetrating NKr antagonists. After demonstrating the potential use for NKr antagonists in animal models, some compounds have recently progressed into clinical trials and a few results have been published. NKr antagonists have demonstrated efficacy for the treatment of emesis and depression, while results in other areas have been disappointing. Nonetheless, this area is coming to the exciting time of proof of concept in humans. Demonstration of the involvement of tachykinin peptides in biological functions continues to grow, as do the potential indications for NKr antagonists. More drug candidates are undergoing clinical trials for various conditions and these results could widen the potential use for NKr antagonists.
Leroy
V
V
Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA.
Mauser
P
P
Gao
Z
Z
Peet
N P
NP
D000818:Animals; D001249:Asthma / Q000188:drug therapy; D002986:Clinical Trials as Topic; D003866:Depressive Disorder / Q000188:drug therapy*; D004195:Disease Models, Animal; D006801:Humans; D018039:Receptors, Tachykinin / Q000037:antagonists & inhibitors*; D015320:Tachykinins / Q000627:therapeutic use*; D014839:Vomiting / Q000517:prevention & control*
D018039:Receptors, Tachykinin; D015320:Tachykinins