Central Nervous System Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Central Nervous System Agents) - Volume 7, Issue 4, 2007

The uridine nucleotides UTP, UDP and UDP-sugars produce a variety of effects by activating specific G protein- coupled P2Y receptors, i.e., the P2Y2, P2Y4, P2Y6 and P2Y14 variants. Except for P2Y14 which has recently been defined, stimulation of P2Y receptors by UTP and/or UDP augments proliferation of adult multipotent neural stem cells; stimulates dopaminergic differentiation in human mesencephalic neural st Read More

An extract from the leaves of the Ginkgo biloba tree, labeled EGb761, is one of the most widely used medicinal products in the West for cardiovascular and brain related diseases. In particular, it has been used frequently for the treatment and prevention of neurodegenerative diseases such as mild cognitive impairment or Alzheimer's disease. The drug is relatively safe and has been used widely by healthy indivi Read More

Proteasomes (including constitutive proteasome, immunoproteasome, and their regulatory complexes) are multicatalytic complexes crucial for cell and body homeostasis and survival, being responsible for a consistent part of protein degradation. In the central nervous system (CNS), the activity of proteasomes affects a variety of crucial brain activities. While proteasome alteration (content and activity) during aging has been stu Read More

After injury to the central nervous system (CNS) of adult vertebrates, axonal regeneration is extremely limited because inhibitory proteins existing around the injury site prevent the regrowth of the lesioned axons. Previous studies have reported that several myelin-derived proteins (such as Nogo, MAG, OMgp) and developmental guidance proteins (such as RGM, semaphorin, ephrin) contribute to the inhibition of axonal regen Read More

Ischaemic stroke is a leading cause of death and disability in the Western world and usually occurs as a consequence of progressing atherothrombosis resulting in embolism and associated local tissue damage due to loss of cell membrane integrity and altered signal transduction activity. Survival of neurones, particularly in peri-infarcted regions determines the extent of patient recovery. A significant proportion of Read More

The high-affinity glycine transporter 1 (GlyT1) is the primary endogenous regulator of glycine levels in the vicinity of the N-methyl-D-aspartate receptor (NMDAR). As a co-agonist, glycine can allosterically modulate NMDAR functions through its binding to the glycine binding site (glycine-B site). Under homeostatic conditions, GlyT1 mediated re-uptake is believed to maintain the synaptic glycine concentration below the satu Read More

A large body of evidence shows that α7 nicotinic acetylcholine receptor (nAChR) is an important mechanism underlying attentional and cognitive deficits in schizophrenia. Several compounds acting as activators of α7 nAChRs have been identified and investigated for a potential therapeutic application. However, considering the complexity of neuropsychiatric disorders and the difficulty to meet an ideal product profile for dru Read More

The CNS is both source and target of melatonin. It is released from the pineal to the circulation and, in elevated concentrations, into the third ventricle. Levels by 3 orders of magnitude higher than in the circulation have been found in the CNS. The mammalian circadian pacemaker, suprachiasmatic nucleus (SCN), controls the pineal, but is also major subject to feedback information on darkness, transduced by two G- Read More