Glutamate receptors as therapeutic targets: present status and future perspectives

• Autorzy: Danysz W.
• Języki publikacji: EN

Abstrakty

EN

In spite of intensive research for over 2 decades, number of drugs affecting glutamatergic system that are clinically used is very limited. This presentation will be devoted to overview of selected glutamate targets, current drug development, their potential and pitfalls. In particular, NMDA receptors (channel blockers and NR2B antagonists) and mGluR5 positive and negative modulators will be discussed more extensively. In case of NMDA receptors, some channel blockers (e.g. memantine) or NR2B antagonists are in clinical use for dementia or are in late stages of development for neuropathic pain respectively. In contrast, mGluR5 modulators are less advanced. Recently, several such substances have been introduced such as MTEP, MPEP, CDPPB or ADX47273. mGluR5 negative allosteric modulators (NAMs) e.g. MTEP are active in some models such as formalin, and Freund adjuvant model of infl ammatory pain. Additionally they have potential in the treatment of L-DOPA induced dyskinesia. mGluR5 positive modulators (PAMs, e.g. CDPPB) may have potential as antipsychotics and improve learning. As it will be presented, in our hands these expectations can be only partially fulfi lled as no clear convincing picture arises from testing in various animal models of schizophrenia (amphetamine-induced hyperactivity or apomorphine-induced prepulse inhibition). In learning models positive effect was seen in object recognition task (spontaneous forgetting).

• Wydawca: -
• Czasopismo: Acta Neurobiologiae Experimentalis
• Rocznik: 2009
• Tom: 69
• Numer: 1
• Opis fizyczny: p.83

Twórcy

autor

Danysz W.

• Merz Pharmaceuticals, Frankfurt am Main, Germany