XXXX receptor ligands as anxiolytics.

@entity13288 @entity2227 @entity2228 @entity19 @entity73 @entity12370 @entity4176 @entity1245 @entity148 @entity143 @entity140 @entity734 @entity2055
The glutamatergic system has received considerable attention over recent years as a potential target for anxiolytic drugs. In spite of the pronounced anxiolytic-like effects of competitive and non-competitive antagonists of @entity143 receptors in animal models of @entity148 , these substances can not be regarded as potential anxiolytic drugs, mainly due to their side-effect profiles (eg, @entity2055 , myorelaxation, @entity73 processes and psychotomimetic effects). Antagonists and partial agonists of the @entity2228 , receptor inhibit function of the @entity143 receptor complex and evoke in animals an anxiolytic-like response. Although data concerning anti- @entity148 -like effects of @entity2228 , receptor antagonists are not very promising, studies are underway to develop new, brain-penetrating agents devoid of side effects. Further developments are necessary to more fully elucidate the possible involvement of @entity140 / @entity4176 receptors in @entity148 . The recent discovery of metabotropic @entity2227 receptors, which modulate the function of the glutamatergic system, offers new hope for discovery of a new generation of anxiolytics. @entity12370 , a highly selective, brain penetrable, noncompetitive mGlu5 receptor antagonist, evokes anxiolytic-like effects in several animal models of @entity148 , remaining remarkably free of side effects. @entity13288 , a selective brain-penetrable group II mGlu receptor agonist, evokes marked anxiolytic-like effects in animal models of @entity148 . @entity13288 causes mild sedation in @entity19 , does not disturb motor coordination and has no potential to cause @entity734 . Therefore mGlu receptor ligands may become the anxiolytics of the future, free from the side effects characteristic of @entity1245 .
